Moclobemide|MAO inhibitor|From DC Chemicals
Moclobemide belongs to a new generation of short-acting, reversible, monoamine oxidase (MAO) inhibitors.
Catlog: DC8086| Product name: Moclobemide| Cas: 71320-77-9| Other names: | Molecule Formula: C13H17ClN2O2| MW: 268.74. Purity: >98%
Price: 100mg: 400 USD; 250mg: 750 USD; 1000mg: 1400 USD
Moclobemide belongs to a new generation of short-acting, reversible, monoamine oxidase (MAO) inhibitors. In vitro (rat brain homogenates) moclobemide inhibits MAO-A selectively with lower potency than many of the reference MAO inhibitors. However, when measured ex vivo in the rat, the potency of moclobemide is similar to that of reference compounds. In vivo the drug induces a dose-dependent, short-lasting (8-16 hr) and preferential inhibition of MAO-A in the brain and both MAO-A and MAO-B inhibition in extracerebral organs (liver, small intestine and kidney). In the extracerebral tissues of the rat moclobemide induces marked peripheral MAO-B inhibition due to rapid and extensive biotransformation of its morpholine ring. The active molecular species is probably the metabolite Ro 16-6491. The moderate MAO-B inhibition measured after moclobemide intake in human platelets indicates that only minor amounts of Ro 16-6491 are formed in humans. Virtually all metabolites of moclobemide so far identified have been tested in vitro and ex vivo in the rat and proved to be either equipotent or, mostly, less effective than moclobemide as MAO-A inhibitors. In liver homogenates of moclobemide-treated rats MAO-A activity recovers during dialysis or simple incubation at 37 degrees C, suggesting a biodegradation of moclobemide and/or the moclobemide-derived active metabolite(s) by MAO itself or a slow dissociation of the active inhibitory species from the enzyme. Similar to other MAO-A inhibitors, moclobemide induces an increase in the rat brain levels of 5-hydroxytryptamine, norepinephrine and dopamine and a concomitant decrease of their deaminated metabolites. These effects are of short duration (8-16 hr) and parallel the time course of MAO-A inhibition. Moclobemide administered subchronically down-regulates beta adrenoceptors as shown by binding experiments with brain cortical membranes using dihydroalprenolol as ligand. In vitro MAO inhibition by moclobemide is specific in that the compound does not affect other amine oxidases or monoamine uptake mechanisms; furthermore, it does not interact with various neurotransmitter or drug receptor sites. In conclusion, a large body of preclinical evidence characterizes moclobemide as a short-acting and reversible MAO-inhibitor. The neurochemical profile of moclobemide indicates clearly that this nonhydrazine nonhepatotoxic MAO-A inhibitor represents a novel and safe drug for treatment of affective disorders.
Moclobemide is a reversible inhibitor of monoamine-oxidase-A (RIMA) and has been extensively evaluated in the treatment of a wide spectrum of depressive disorders and less extensively studied in anxiety disorders. Nearly all meta-analyses and most comparative studies indicated that in the acute management of depression this drug is more efficacious than placebo and as efficacious as tricyclic (or some heterocyclic) antidepressants or selective serotonin reuptake inhibitors (SSRIs). There is a growing evidence that moclobemide is not inferior to other antidepressants in the treatment of subtypes of depression, such as dysthymia, endogenous (unipolar and bipolar), reactive, atypical, agitated, and retarded depression as with other antidepressants limited evidence suggests that moclobemide has consistent long-term efficacy. However, more controlled studies addressing this issue are needed. For patients with bipolar depression the risk of developing mania seems to be not higher with moclobemide than with other antidepressants. The effective therapeutic dose range for moclobemide in most acute phase trials was 300 to 600 mg, divided in 2 to 3 doses. While one controlled trial and one long-term open-label study found moclobemide to be efficacious in social phobia, three controlled trials subsequently revealed either no effect or less robust effects with the tendency of higher doses (600 - 900 mg/d) to be more efficacious. Two comparative trials demonstrated moclobemide to be as efficacious as fluoxetine or clomipramine in patients suffering from panic disorder. Placebo-controlled trials in this indication are, however, still lacking. A relationship between the plasma concentration of moclobemide and its therapeutic efficacy is not apparent but a positive correlation with adverse events has been found. Dizziness, nausea and insomnia occurred more frequently on moclobemide than on placebo. Due to negligible anticholinergic and antihistaminic actions, moclobemide has been better tolerated than tri- or heterocyclic antidepressants. Gastrointestinal side effects and, especially, sexual dysfunction were much less frequent with moclobemide than with SSRIs. Unlike irreversible MAO-inhibitors, moclobemide has a negligible propensity to induce hypertensive crisis after ingestion of tyramine-rich food ("cheese-reaction"). Therefore, dietary restrictions are not as strict. However, with moclobemide doses above 900 mg/d the risk of interaction with ingested tyramine might become clinically relevant. After multiple dosing the oral bioavailability of moclobemide reaches almost 100%. At therapeutic doses, moclobemide lacks significant negative effects on psychomotor performance, cognitive function or cardiovascular system. Due to the relative freedom from these side effects, moclobemide is particularly attractive in the treatment of elderly patients. Moclobemide is a substrate of CYP2C19. Although it acts as an inhibitor of CYP1A2, CYP2C19, and CYP2D6, relatively few clinically important drug interactions involving moclobemide have been reported. It is relatively safe even in overdose. The drug has a short plasma elimination half-life that allows switching to an alternative agent within 24 h. Since it is well tolerated, therapeutic doses can often be reached rapidly upon onset of treatment. Steady-state plasma levels are reached approximately at one week following dose adjustment. Patients with renal dysfunction require no dose reduction in contrast to patients with severe hepatic impairment. Cases of refractory depression might improve with a combination of moclobemide with other antidepressants, such as clomipramine or a SSRI. Since this combination has rarely been associated with a potentially lethal serotonin syndrome, it requires lower entry doses, a slower dose titration and a more careful monitoring of patients. Combination therapy with moclobemide and other serotonergic agents, or opioids, should be undertaken with caution, although no serious adverse events have been published with therapeutic doses of moclobemide to date
For research and scientific purpose only, not for human use.
2015年5月31日星期日
Fexaramine|FXR activator|DC Chemicals
Fexaramine|FXR activator|DC Chemicals
Fexaramine is a potent, selective FXR activator.
Catlog: DC8085| Product name: Fexaramine| Cas: 574013-66-4| Other names: Fexaramine| Molecule Formula: C32H36N2O3| MW: 496.64. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
Fexaramine is a potent, selective FXR (farnesoid X receptor) agonist (EC50 = 25 nM). Fexaramine displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors.
For research and scientific purpose only, not for human use.
Fexaramine is a potent, selective FXR activator.
Catlog: DC8085| Product name: Fexaramine| Cas: 574013-66-4| Other names: Fexaramine| Molecule Formula: C32H36N2O3| MW: 496.64. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
Fexaramine is a potent, selective FXR (farnesoid X receptor) agonist (EC50 = 25 nM). Fexaramine displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors.
For research and scientific purpose only, not for human use.
kb NB 142-70|PKD inhibitor|DC Chemicals
kb NB 142-70|PKD inhibitor|DC Chemicals
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor.
Catlog: DC8084| Product name: kb NB 142-70| Cas: 1233533-04-4| Other names: | Molecule Formula: C11H9NO2S2| MW: 251.32. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor. Demonstrates a 7-fold increase in inhibition potency as an analog of CID 755673. Reported to demonstrate prominent cytotoxic and anti-proliferative effects in vitro. Additionally noted to inhibit cell migration and invasion in a prostate cancer cell line. kb NB 142-70 is an inhibitor of PKC μ, PKC ν and PKD2.
For research and scientific purpose only, not for human use.
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor.
Catlog: DC8084| Product name: kb NB 142-70| Cas: 1233533-04-4| Other names: | Molecule Formula: C11H9NO2S2| MW: 251.32. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor. Demonstrates a 7-fold increase in inhibition potency as an analog of CID 755673. Reported to demonstrate prominent cytotoxic and anti-proliferative effects in vitro. Additionally noted to inhibit cell migration and invasion in a prostate cancer cell line. kb NB 142-70 is an inhibitor of PKC μ, PKC ν and PKD2.
For research and scientific purpose only, not for human use.
NS11394（NS 11394）GABAA receptor modulator|DC Chemicals
NS11394（NS 11394）GABAA receptor modulator|DC Chemicals
NS11394 possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
Catlog: DC8083| Product name: NS11394| Cas: 951650-22-9| Other names: NS 11394,NS-11394，NS11394| Molecule Formula: C23H19N3O| MW: 353.42. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil. Ongoing inflammatory nociception, observed as hindpaw weight-bearing deficits after Freund's adjuvant injection, was also completely reversed by NS11394. Likewise, hindpaw mechanical allodynia was fully reversed by NS11394 in two rat models of peripheral neuropathic pain. Importantly, NS11394-mediated antinociception occurred at doses 20 to 40-fold lower than those inducing minor sedative or ataxic impairments. In contrast, putative antinociception associated with administration of either diazepam, zolpidem, or gaboxadol only occurred at doses producing intolerable side effects, whereas bretazenil was completely inactive despite minor influences on motoric function. In electrophysiological studies, NS11394 selectively attenuated spinal nociceptive reflexes and C-fiber-mediated wind-up in vitro pointing to involvement of a spinal site of action. The robust therapeutic window seen with NS11394 in animals suggests that compounds with this in vitro selectivity profile could have potential benefit in clinical treatment of pain in humans.
For research and scientific purpose only, not for human use.
NS11394 possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
Catlog: DC8083| Product name: NS11394| Cas: 951650-22-9| Other names: NS 11394,NS-11394，NS11394| Molecule Formula: C23H19N3O| MW: 353.42. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil. Ongoing inflammatory nociception, observed as hindpaw weight-bearing deficits after Freund's adjuvant injection, was also completely reversed by NS11394. Likewise, hindpaw mechanical allodynia was fully reversed by NS11394 in two rat models of peripheral neuropathic pain. Importantly, NS11394-mediated antinociception occurred at doses 20 to 40-fold lower than those inducing minor sedative or ataxic impairments. In contrast, putative antinociception associated with administration of either diazepam, zolpidem, or gaboxadol only occurred at doses producing intolerable side effects, whereas bretazenil was completely inactive despite minor influences on motoric function. In electrophysiological studies, NS11394 selectively attenuated spinal nociceptive reflexes and C-fiber-mediated wind-up in vitro pointing to involvement of a spinal site of action. The robust therapeutic window seen with NS11394 in animals suggests that compounds with this in vitro selectivity profile could have potential benefit in clinical treatment of pain in humans.
For research and scientific purpose only, not for human use.
CZC-54252(CZC54252)|LRRK2 inhibitor|DC Chemicals
CZC-54252(CZC54252)|LRRK2 inhibitor|DC Chemicals
CZC-54252 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) (IC50 values are 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively).
Catlog: DC8082| Product name: CZC-54252| Cas: 1191911-27-9| Other names: CZC 54252,CZC54252| Molecule Formula: C22H25ClN6O4S| MW: 504.99. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
For research and scientific purpose only, not for human use.
CZC-54252 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) (IC50 values are 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively).
Catlog: DC8082| Product name: CZC-54252| Cas: 1191911-27-9| Other names: CZC 54252,CZC54252| Molecule Formula: C22H25ClN6O4S| MW: 504.99. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1000 USD; 1000mg: 1800 USD
For research and scientific purpose only, not for human use.
WHI-P258|JAK3 Inhibitor Negative Control|DC Chemicals
WHI-P258|JAK3 Inhibitor Negative Control|DC Chemicals
WHI-P258 is a negative control for JAK3 inhibitors.
Catlog: DC8080| Product name: WHI-P258| Cas: 21561-09-1| Other names: JAK3 Inhibitor Negative Control,WHIP258,WHI P258| Molecule Formula: C16H15N3O2| MW: 281.31. Purity: >98%
Price: 100mg: 500 USD; 250mg: 850 USD; 1000mg: 1600 USD
The JAK3 Inhibitor, Negative Control, also referenced under CAS 153437-07-1, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
For research and scientific purpose only, not for human use.
WHI-P258 is a negative control for JAK3 inhibitors.
Catlog: DC8080| Product name: WHI-P258| Cas: 21561-09-1| Other names: JAK3 Inhibitor Negative Control,WHIP258,WHI P258| Molecule Formula: C16H15N3O2| MW: 281.31. Purity: >98%
Price: 100mg: 500 USD; 250mg: 850 USD; 1000mg: 1600 USD
The JAK3 Inhibitor, Negative Control, also referenced under CAS 153437-07-1, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
For research and scientific purpose only, not for human use.
AG-1557(AG1557) cas 189290-58-2|DC Chemicals
AG-1557(AG1557) cas 189290-58-2|DC Chemicals
AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).
Catlog: DC8079| Product name: AG-1557| Cas: 189290-58-2| Other names: AG 1557,AG1557 | Molecule Formula: C16H14IN3O2| MW: 407.211. Purity: >98%
Price: 100mg: 500 USD; 250mg: 850 USD; 1000mg: 1600 USD
AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).
For research and scientific purpose only, not for human use.
AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).
Catlog: DC8079| Product name: AG-1557| Cas: 189290-58-2| Other names: AG 1557,AG1557 | Molecule Formula: C16H14IN3O2| MW: 407.211. Purity: >98%
Price: 100mg: 500 USD; 250mg: 850 USD; 1000mg: 1600 USD
AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).
For research and scientific purpose only, not for human use.
PD 153035(AG-1517)|EGFR inhibitor|DC Chemicasl
PD 153035(AG-1517)|EGFR inhibitor|DC Chemicasl
PD 153035(AG-1517) is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK), with an IC50 of 25 pM.
Catlog: DC8078| Product name: PD 153035(AG-1517)| Cas: 153436-54-5| Other names: PD153035，AG1517，PD-153035，AG-1517| Molecule Formula: C16H14BrN3O2| MW: 360.21. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
An ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK), with an IC50 of 25 pM. Inhibits other tyrosine kinases at micromolar or higher concentrations. It selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression and oncogenic transformation. Inhibits the growth of a number of cancer cell lines. An extremely useful tool for exploring EGF-mediated cellular signaling.
For research and scientific purpose only, not for human use.
PD 153035(AG-1517) is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK), with an IC50 of 25 pM.
Catlog: DC8078| Product name: PD 153035(AG-1517)| Cas: 153436-54-5| Other names: PD153035，AG1517，PD-153035，AG-1517| Molecule Formula: C16H14BrN3O2| MW: 360.21. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
An ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK), with an IC50 of 25 pM. Inhibits other tyrosine kinases at micromolar or higher concentrations. It selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression and oncogenic transformation. Inhibits the growth of a number of cancer cell lines. An extremely useful tool for exploring EGF-mediated cellular signaling.
For research and scientific purpose only, not for human use.
WHI-P131(Janex 1)
WHI-P131(Janex 1)|DC Chemicals
Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).
Catlog: DC8077| Product name: WHI-P131(Janex 1)| Cas: 202475-60-3| Other names: WHIP-131,Janex-1)，WHIP131,Janex1| Molecule Formula: C16H15N3O3| MW: 297.31. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).Janex 1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.
For research and scientific purpose only, not for human use.
Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).
Catlog: DC8077| Product name: WHI-P131(Janex 1)| Cas: 202475-60-3| Other names: WHIP-131,Janex-1)，WHIP131,Janex1| Molecule Formula: C16H15N3O3| MW: 297.31. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).Janex 1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.
For research and scientific purpose only, not for human use.
NG 52 (Compound 52)|cell cycle kinase inhibitor
NG 52 (Compound 52)|cell cycle kinase inhibitor|DC Chemicals
NG 52 (Compound 52) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).
Catlog: DC8076| Product name: NG 52 (Compound 52 )| Cas: 212779-48-1| Other names: NG52, Compound52,NG-52,Compound-52| Molecule Formula: C16H19ClN6O| MW: 346.81. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
NG 52 (Compound 52 ) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).
For research and scientific purpose only, not for human use.
NG 52 (Compound 52) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).
Catlog: DC8076| Product name: NG 52 (Compound 52 )| Cas: 212779-48-1| Other names: NG52, Compound52,NG-52,Compound-52| Molecule Formula: C16H19ClN6O| MW: 346.81. Purity: >98%
Price: 100mg: 350 USD; 250mg: 650 USD; 1000mg: 1300 USD
NG 52 (Compound 52 ) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).
For research and scientific purpose only, not for human use.
Purvalanol A(NG 60)|CDK inhibitor|DC Chemicals
Purvalanol A(NG 60)|CDK inhibitor|DC Chemicals
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.
Catlog: DC8075| Product name: Purvalanol A(NG 60)| Cas: 212844-53-6| Other names: NG 60,NG60,NG-60| Molecule Formula: C19H25ClN6O| MW: 388.89. Purity: >98%
Price: 100mg: 550 USD; 250mg: 950 USD; 1000mg: 1800 USD
Purvalanol A is a potent, cell-permeable, and selective inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively. Purvalanol A reversibly arrests synchronized cells in the G1 and G2 phase of the cell cycle, inhibiting both cell proliferation and cell death.At 10 μM, purvalanol A potently suppresses the anchorage-independent growth of c-Src-transformed cells as well as HT29 and SW48 human colon cancer cells.
For research and scientific purpose only, not for human use.
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.
Catlog: DC8075| Product name: Purvalanol A(NG 60)| Cas: 212844-53-6| Other names: NG 60,NG60,NG-60| Molecule Formula: C19H25ClN6O| MW: 388.89. Purity: >98%
Price: 100mg: 550 USD; 250mg: 950 USD; 1000mg: 1800 USD
Purvalanol A is a potent, cell-permeable, and selective inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively. Purvalanol A reversibly arrests synchronized cells in the G1 and G2 phase of the cell cycle, inhibiting both cell proliferation and cell death.At 10 μM, purvalanol A potently suppresses the anchorage-independent growth of c-Src-transformed cells as well as HT29 and SW48 human colon cancer cells.
For research and scientific purpose only, not for human use.
MHY1485（MHY 1485| mTOR activator|DC Chemicals
MHY1485（MHY 1485| mTOR activator|DC Chemicals
MHY1485 is mTOR activator that potently inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
Catlog: DC8074| Product name: MHY1485| Cas: 326914-06-1| Other names: MHY-1485，MHY 1485| Molecule Formula: C17H21N7O4| MW: 387.39314. Purity: >98%
Price: 100mg: 400 USD; 250mg: 750 USD; 1000mg: 1400 USD
MHY1485, in a culture system by using Ac2F rat hepatocytes. Autophagic flux was measured to evaluate the autophagic activity. Autophagosomes were visualized in Ac2F cells transfected with AdGFP-LC3 by live-cell confocal microscopy. In addition, activity of mTOR, a major regulatory protein of autophagy, was assessed by western blot and docking simulation using AutoDock 4.2. In the result, treatment with MHY1485 suppressed the basal autophagic flux, and this inhibitory effect was clearly confirmed in cells under starvation, a strong physiological inducer of autophagy. The levels of p62 and beclin-1 did not show significant change after treatment with MHY1485. Decreased co-localization of autophagosomes and lysosomes in confocal microscopic images revealed the inhibitory effect of MHY1485 on lysosomal fusion during starvation-induced autophagy. These effects of MHY1485 led to the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time- dependent manner. Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound. The significance of this study is the finding of a novel inhibitor of autophagy with an mTOR activating effect.
For research and scientific purpose only, not for human use.
MHY1485 is mTOR activator that potently inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
Catlog: DC8074| Product name: MHY1485| Cas: 326914-06-1| Other names: MHY-1485，MHY 1485| Molecule Formula: C17H21N7O4| MW: 387.39314. Purity: >98%
Price: 100mg: 400 USD; 250mg: 750 USD; 1000mg: 1400 USD
MHY1485, in a culture system by using Ac2F rat hepatocytes. Autophagic flux was measured to evaluate the autophagic activity. Autophagosomes were visualized in Ac2F cells transfected with AdGFP-LC3 by live-cell confocal microscopy. In addition, activity of mTOR, a major regulatory protein of autophagy, was assessed by western blot and docking simulation using AutoDock 4.2. In the result, treatment with MHY1485 suppressed the basal autophagic flux, and this inhibitory effect was clearly confirmed in cells under starvation, a strong physiological inducer of autophagy. The levels of p62 and beclin-1 did not show significant change after treatment with MHY1485. Decreased co-localization of autophagosomes and lysosomes in confocal microscopic images revealed the inhibitory effect of MHY1485 on lysosomal fusion during starvation-induced autophagy. These effects of MHY1485 led to the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time- dependent manner. Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound. The significance of this study is the finding of a novel inhibitor of autophagy with an mTOR activating effect.
For research and scientific purpose only, not for human use.
Bohemine|CDK inhibitor|DC Chemicals
Bohemine|CDK inhibitor|DC Chemicals
Bohemine is a synthetic, cell-permeable, cyclin-dependent kinase inhibitor.
Catlog: DC8073| Product name: Bohemine| Cas: 189232-42-6| Other names: N/A| Molecule Formula: C18H24N6O| MW: 340.4. Purity: >98%
Price: 100mg: 700 USD; 250mg: 1200 USD; 1000mg: 2200 USD
Bohemine is a cell permeable inhibitor of CDK1 (IC50=1.1µM) and CD2 (IC50=600nM). Bohemine is structurally similar to Olomoucine and Roscovitine . Arrests cell cycle in the G1/S boundary and activates in vitro matured bovine oocytes either alone or in combination with Ionomycin.
For research and scientific purpose only, not for human use.
Bohemine is a synthetic, cell-permeable, cyclin-dependent kinase inhibitor.
Catlog: DC8073| Product name: Bohemine| Cas: 189232-42-6| Other names: N/A| Molecule Formula: C18H24N6O| MW: 340.4. Purity: >98%
Price: 100mg: 700 USD; 250mg: 1200 USD; 1000mg: 2200 USD
Bohemine is a cell permeable inhibitor of CDK1 (IC50=1.1µM) and CD2 (IC50=600nM). Bohemine is structurally similar to Olomoucine and Roscovitine . Arrests cell cycle in the G1/S boundary and activates in vitro matured bovine oocytes either alone or in combination with Ionomycin.
For research and scientific purpose only, not for human use.
Altiratinib(DCC-2701)|Multi Kinase Inhibitor|From DC Chemcials
Altiratinib(DCC-2701)|Multi Kinase Inhibitor|From DC Chemcials
Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.
Catlog: DC8072| Product name: Altiratinib(DCC-2701)| Cas: 1345847-93-9| Other names: Altiratinib, DCC2701,DCC 2701| Molecule Formula: C26H21F3N4O4| MW: 510.15. Purity: >98%
Price: 100mg: 700 USD; 250mg: 1200 USD; 1000mg: 2200 USD
Altiratinib (DCC-2701) provided balanced inhibition of MET, TRK, TIE2 and VEGFR2 kinases. Altiratinib exhibited potency against both wild-type and mutant forms of MET and TRK kinases. In in vivo studies, altiratinib was shown to inhibit tumor growth, evasive vascularization, invasion and/or metastasis. In one model an increased overall survival was observed. Altiratinib exhibited anti-tumor activity in a variety of xenograft or allograft tumor models, including melanoma, gastric, lung, colorectal, breast, ovarian and glioblastoma. Altiratinib is currently in a Phase 1 clinical study in cancer patients with solid tumors.Altiratinib potently inhibited MET, TIE2, VEGFR2, and TRK kinases in functional cellular assays, including activity against proliferation, migration, and capillary tube formation, and with sufficient single-digit nanomolar potency such that all of these targets could be effectively inhibited simultaneously in vivo.Altiratinib exhibited efficacy at preventing tumor growth, as well as inhibiting evasive vascularization, pro-tumoral macrophages, epithelial-to-mesenchymal transition (EMT) and metastasis in a variety of cancer models.Altiratinib inhibited MET kinase for more than 24 hours after a single 10 mg/kg dose in a gastric cancer xenograft model leading to significant inhibition of tumor growth.Altiratinib blocked bevacizumab-induced evasive vascularization and EMT in an aggressive, invasive glioblastoma model.Altiratinib inhibited primary tumor growth and showed additive activity with paclitaxel; in addition, it reduced TIE2-expressing macrophages in the tumor stroma and significantly reduced lung metastases in a metastatic breast cancer model.Altiratinib exhibited a long off-rate from kinases (greater than 24 hours from TIE2 and TRKA) in a variety of cell-based assays, based on its binding mode.Altiratinib inhibited microvessel density and tumor growth in a xenograft model where both TIE2 and VEGFR2 kinases contribute to vessel growth.Altiratinib compared favorably with other multi-targeted MET inhibitors, and had additional activity in inhibiting oncogenic MET mutants found in papillary renal cell carcinoma (PRCC), while other MET inhibitors have not been shown to inhibit activated MET mutants.
For research and scientific purpose only, not for human use.
Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.
Catlog: DC8072| Product name: Altiratinib(DCC-2701)| Cas: 1345847-93-9| Other names: Altiratinib, DCC2701,DCC 2701| Molecule Formula: C26H21F3N4O4| MW: 510.15. Purity: >98%
Price: 100mg: 700 USD; 250mg: 1200 USD; 1000mg: 2200 USD
Altiratinib (DCC-2701) provided balanced inhibition of MET, TRK, TIE2 and VEGFR2 kinases. Altiratinib exhibited potency against both wild-type and mutant forms of MET and TRK kinases. In in vivo studies, altiratinib was shown to inhibit tumor growth, evasive vascularization, invasion and/or metastasis. In one model an increased overall survival was observed. Altiratinib exhibited anti-tumor activity in a variety of xenograft or allograft tumor models, including melanoma, gastric, lung, colorectal, breast, ovarian and glioblastoma. Altiratinib is currently in a Phase 1 clinical study in cancer patients with solid tumors.Altiratinib potently inhibited MET, TIE2, VEGFR2, and TRK kinases in functional cellular assays, including activity against proliferation, migration, and capillary tube formation, and with sufficient single-digit nanomolar potency such that all of these targets could be effectively inhibited simultaneously in vivo.Altiratinib exhibited efficacy at preventing tumor growth, as well as inhibiting evasive vascularization, pro-tumoral macrophages, epithelial-to-mesenchymal transition (EMT) and metastasis in a variety of cancer models.Altiratinib inhibited MET kinase for more than 24 hours after a single 10 mg/kg dose in a gastric cancer xenograft model leading to significant inhibition of tumor growth.Altiratinib blocked bevacizumab-induced evasive vascularization and EMT in an aggressive, invasive glioblastoma model.Altiratinib inhibited primary tumor growth and showed additive activity with paclitaxel; in addition, it reduced TIE2-expressing macrophages in the tumor stroma and significantly reduced lung metastases in a metastatic breast cancer model.Altiratinib exhibited a long off-rate from kinases (greater than 24 hours from TIE2 and TRKA) in a variety of cell-based assays, based on its binding mode.Altiratinib inhibited microvessel density and tumor growth in a xenograft model where both TIE2 and VEGFR2 kinases contribute to vessel growth.Altiratinib compared favorably with other multi-targeted MET inhibitors, and had additional activity in inhibiting oncogenic MET mutants found in papillary renal cell carcinoma (PRCC), while other MET inhibitors have not been shown to inhibit activated MET mutants.
For research and scientific purpose only, not for human use.
Fexarine,cas 574013-67-5|farnesoid X receptor agonist
Fexarine,cas 574013-67-5|farnesoid X receptor agonist|DC Chemicals
Fexarine is a potent, selective farnesoid X receptor agonist.
Catlog: DC8071| Product name: Fexarine| Cas: 574013-67-5| Other names: | Molecule Formula: C31H31NO6| MW: 497.22. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexarine is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
Fexarine is a potent, selective farnesoid X receptor agonist.
Catlog: DC8071| Product name: Fexarine| Cas: 574013-67-5| Other names: | Molecule Formula: C31H31NO6| MW: 497.22. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexarine is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
Fexarene,cas 574013-68-6|farnesoid X receptor agonist
Fexarene,cas 574013-68-6|farnesoid X receptor agonist|DC Chemicals
Fexarene is a potent, selective farnesoid X receptor agonist.
Catlog: DC8070| Product name: Fexarene| Cas: 574013-68-6| Other names: | Molecule Formula: C32H33N03| MW: 479.61. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexarene is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
Fexarene is a potent, selective farnesoid X receptor agonist.
Catlog: DC8070| Product name: Fexarene| Cas: 574013-68-6| Other names: | Molecule Formula: C32H33N03| MW: 479.61. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexarene is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
Fexaramate,cas 592524-75-9|farnesoid X receptor agonist
Fexaramate,cas 592524-75-9|farnesoid X receptor agonist |DC Chemicals
Fexaramate is a potent, selective farnesoid X receptor agonist.
Catlog: DC8069| Product name: Fexaramate| Cas: 592524-75-9| Other names: | Molecule Formula: C31H37NO5| MW: 503.27. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexaramate is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
Fexaramate is a potent, selective farnesoid X receptor agonist.
Catlog: DC8069| Product name: Fexaramate| Cas: 592524-75-9| Other names: | Molecule Formula: C31H37NO5| MW: 503.27. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1100 USD; 1000mg: 2000 USD
Fexaramate is a potent, selective farnesoid X receptor agonist.
For research and scientific purpose only, not for human use.
WHI-P180(Janex 3)|EGFR/CDK2 inhibitor|DC Chemicals
WHI-P180(Janex 3)|EGFR/CDK2 inhibitor|DC Chemicals
WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site
Catlog: DC8068| Product name: WHI-P180(Janex 3)| Cas: 211555-08-7| Other names: WHI P180,Janex3,WHIP180,Janex-3| Molecule Formula: C16H15N3O3| MW: 297.31. Purity: >98%
Price: 100mg: 450 USD; 250mg: 850 USD; 1000mg: 1600 USD
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
in vitro: WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity.
in vivo: The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o. administration was less than 10 min. Systemic clearance of WHI-P180 was 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis.
For research and scientific purpose only, not for human use.
WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site
Catlog: DC8068| Product name: WHI-P180(Janex 3)| Cas: 211555-08-7| Other names: WHI P180,Janex3,WHIP180,Janex-3| Molecule Formula: C16H15N3O3| MW: 297.31. Purity: >98%
Price: 100mg: 450 USD; 250mg: 850 USD; 1000mg: 1600 USD
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
in vitro: WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity.
in vivo: The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o. administration was less than 10 min. Systemic clearance of WHI-P180 was 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis.
For research and scientific purpose only, not for human use.
Cefozopran (SCE-2787)|cas 113359-04-9|DC Chemicals
Cefozopran (SCE-2787)|cas 113359-04-9|DC Chemicals
Cefozopran (SCE-2787) is a new parenteral cephalosporin, against experimental infections in mice.
Catlog: DC8067| Product name: Cefozopran(SCE 2787)| Cas: 113359-04-9| Other names: SCE2787,SCE 2787| Molecule Formula: C19H17N9O5S2| MW: 515.52. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1800 USD
efozopran (SCE-2787) is a new semisynthetic parenteral cephalosporin, against experimental infections in mice was examined. Cefozopran was more effective than cefpiramide and was as effective as ceftazidime and cefpirome against acute respiratory tract infections caused by Klebsiella pneumoniae DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, cefozopran was as effective as ceftazidime. The therapeutic effect of cefozopran against urinary tract infections caused by Pseudomonas aeruginosa P9 was superior to that of cefpirome and was equal to those of ceftazidime and cefclidin. In addition, cefozopran was more effective than ceftazidime and was as effective as flomoxef in a thigh muscle infection caused by methicillin-sensitive Staphylococcus aureus 308A-1. Against thigh muscle infections caused by methicillin-resistant S. aureus N133, cefozopran was the most effective agent. The potent therapeutic effect of cefozopran in those experimental infections in mice suggests that it would be effective against respiratory tract, urinary tract, and soft tissue infections caused by a variety of gram-positive and gram-negative bacteria in humans.
For research and scientific purpose only, not for human use.
Cefozopran (SCE-2787) is a new parenteral cephalosporin, against experimental infections in mice.
Catlog: DC8067| Product name: Cefozopran(SCE 2787)| Cas: 113359-04-9| Other names: SCE2787,SCE 2787| Molecule Formula: C19H17N9O5S2| MW: 515.52. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1800 USD
efozopran (SCE-2787) is a new semisynthetic parenteral cephalosporin, against experimental infections in mice was examined. Cefozopran was more effective than cefpiramide and was as effective as ceftazidime and cefpirome against acute respiratory tract infections caused by Klebsiella pneumoniae DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, cefozopran was as effective as ceftazidime. The therapeutic effect of cefozopran against urinary tract infections caused by Pseudomonas aeruginosa P9 was superior to that of cefpirome and was equal to those of ceftazidime and cefclidin. In addition, cefozopran was more effective than ceftazidime and was as effective as flomoxef in a thigh muscle infection caused by methicillin-sensitive Staphylococcus aureus 308A-1. Against thigh muscle infections caused by methicillin-resistant S. aureus N133, cefozopran was the most effective agent. The potent therapeutic effect of cefozopran in those experimental infections in mice suggests that it would be effective against respiratory tract, urinary tract, and soft tissue infections caused by a variety of gram-positive and gram-negative bacteria in humans.
For research and scientific purpose only, not for human use.
Loxiglumide|CCK-A antagonist|DC Chemicals
Loxiglumide|CCK-A antagonist|DC Chemicals
Loxiglumide is a Exogenous cholecystokinin (CCK-A) receptor antagonist, stimulates calorie intake and hunger feelings in humans.
Catlog: DC8066| Product name: Loxiglumide| Cas: 107097-80-3| Other names: | Molecule Formula: C21H30Cl2N2O5| MW: 461.38. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1900 USD
Loxiglumide is a small-molecule antagonist of the cholecystokinin receptor CCKA. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.
For research and scientific purpose only, not for human use.
Loxiglumide is a Exogenous cholecystokinin (CCK-A) receptor antagonist, stimulates calorie intake and hunger feelings in humans.
Catlog: DC8066| Product name: Loxiglumide| Cas: 107097-80-3| Other names: | Molecule Formula: C21H30Cl2N2O5| MW: 461.38. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1900 USD
Loxiglumide is a small-molecule antagonist of the cholecystokinin receptor CCKA. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.
For research and scientific purpose only, not for human use.
LY-2409881(LY2409881)|IKK2 inhibitor|From DC Chemicals
LY-2409881(LY2409881)|IKK2 inhibitor|From DC Chemicals
LY2409881 is a novel inhibitor of IκB kinase β (IKK2).
Catlog: DC8065| Product name: LY2409881 trihydrochloride| Cas: 946518-60-1| Other names: LY-2409881 ,LY 2409881 | Molecule Formula: C24H32Cl4N6OS| MW: 594.43. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1900 USD
LY2409881 is a novel inhibitor of IκB kinase β (IKK2). LY2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. In models of diffuse large B-cell lymphoma (DLBCL), the cytotoxicity of LY2409881 correlated with the overall activation status of NF-κB, but not simply in a pattern predicted by the cell-of-origin classification of these cell lines. LY2409881 was safe to mice at three dose levels, 50, 100, and 200 mg/kg, all of which caused significant inhibition of tumor growth. LY2409881 suppressed the activity of the NF-κB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs.
For research and scientific purpose only, not for human use.
LY2409881 is a novel inhibitor of IκB kinase β (IKK2).
Catlog: DC8065| Product name: LY2409881 trihydrochloride| Cas: 946518-60-1| Other names: LY-2409881 ,LY 2409881 | Molecule Formula: C24H32Cl4N6OS| MW: 594.43. Purity: >98%
Price: 100mg: 550 USD; 250mg: 1000 USD; 1000mg: 1900 USD
LY2409881 is a novel inhibitor of IκB kinase β (IKK2). LY2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. In models of diffuse large B-cell lymphoma (DLBCL), the cytotoxicity of LY2409881 correlated with the overall activation status of NF-κB, but not simply in a pattern predicted by the cell-of-origin classification of these cell lines. LY2409881 was safe to mice at three dose levels, 50, 100, and 200 mg/kg, all of which caused significant inhibition of tumor growth. LY2409881 suppressed the activity of the NF-κB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs.
For research and scientific purpose only, not for human use.
AI-10-49 | CBFβ-SMMHC inhibitor|DC Chemicals
AI-10-49 | CBFβ-SMMHC inhibitor|DC Chemicals
AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1.
Catlog: DC8064| Product name: AI-10-49| Cas: 1256094-72-0| Other names: AI 1049,AI1049 | Molecule Formula: C30H22F6N6O5| MW: 660.52. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 2100 USD
AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death.
For research and scientific purpose only, not for human use.
AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1.
Catlog: DC8064| Product name: AI-10-49| Cas: 1256094-72-0| Other names: AI 1049,AI1049 | Molecule Formula: C30H22F6N6O5| MW: 660.52. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 2100 USD
AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death.
For research and scientific purpose only, not for human use.
T-00127-HEV1|PIK inhibitor|DC Chemicals
T-00127-HEV1|PIK inhibitor|DC Chemicals
T-00127-HEV1 is a novel potent phosphoinositide kinases (PIK) inhibitor,T-00127-HEV1 inhibited PI4KB activity with a higher specificity for than other PI kinases.
Catlog: DC8063| Product name: T-00127-HEV1| Cas: 900874-91-1| Other names: T00127-HEV1,T 00127 HEV1| Molecule Formula: C22H29N5O3| MW: 411.5. Purity: >98%
Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1800 USD
T-00127-HEV1 inhibited PI4KB activity with a higher specificity for than other PI kinases, in contrast to GW5074, which had a broad specificity for PI . T-00127-HEV1 and GW5074 did not inhibit hepatitis C virus (HCV) replication, in contrast to a strong inhibitory effect of AN-12-H5. PI4KB is an enterovirus-specific host factor required for the replication process and targeted by some enviroxime-like compounds (T-00127-HEV1 and GW5074) and that enviroxime-like compounds may have targets other than PI kinases for their antiviral effect.
For research and scientific purpose only, not for human use.
T-00127-HEV1 is a novel potent phosphoinositide kinases (PIK) inhibitor,T-00127-HEV1 inhibited PI4KB activity with a higher specificity for than other PI kinases.
Catlog: DC8063| Product name: T-00127-HEV1| Cas: 900874-91-1| Other names: T00127-HEV1,T 00127 HEV1| Molecule Formula: C22H29N5O3| MW: 411.5. Purity: >98%
Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1800 USD
T-00127-HEV1 inhibited PI4KB activity with a higher specificity for than other PI kinases, in contrast to GW5074, which had a broad specificity for PI . T-00127-HEV1 and GW5074 did not inhibit hepatitis C virus (HCV) replication, in contrast to a strong inhibitory effect of AN-12-H5. PI4KB is an enterovirus-specific host factor required for the replication process and targeted by some enviroxime-like compounds (T-00127-HEV1 and GW5074) and that enviroxime-like compounds may have targets other than PI kinases for their antiviral effect.
For research and scientific purpose only, not for human use.
BX517(BX 517)|PDK1 inhibitor|DC Chemicals
BX517(BX 517)|PDK1 inhibitor|DC Chemicals
BX517 is a novel phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
Catlog: DC8062| Product name: BIX517| Cas: 850717-64-5| Other names: BIX-517,BIX 517| Molecule Formula: C15H14N4O2| MW: 282.297. Purity: >98%
Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1800 USD
BX517 is a novel phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
For research and scientific purpose only, not for human use.
BX517 is a novel phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
Catlog: DC8062| Product name: BIX517| Cas: 850717-64-5| Other names: BIX-517,BIX 517| Molecule Formula: C15H14N4O2| MW: 282.297. Purity: >98%
Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1800 USD
BX517 is a novel phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
For research and scientific purpose only, not for human use.
SGC 707(SGC707)|PRMT-3 INHIBITOR|DC Chemicals
SGC 707(SGC707)|PRMT-3 INHIBITOR|DC Chemicals
SGC 707 is a potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) (IC50 = 31 nM).
Catlog: DC8061| Product name: SGC-707| Cas: N/A| Other names: SGC 707,SGC707| Molecule Formula: C16H18N4O2| MW: 298.34. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
Potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) (IC50 = 31 nM). Inhibits PRMT3-mediated methyltransferase activity in vitro. Displays >100-fold selectivity against 31 other methyltransferases and 250 other non-epigenetic targets.
For research and scientific purpose only, not for human use.
SGC 707 is a potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) (IC50 = 31 nM).
Catlog: DC8061| Product name: SGC-707| Cas: N/A| Other names: SGC 707,SGC707| Molecule Formula: C16H18N4O2| MW: 298.34. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
Potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) (IC50 = 31 nM). Inhibits PRMT3-mediated methyltransferase activity in vitro. Displays >100-fold selectivity against 31 other methyltransferases and 250 other non-epigenetic targets.
For research and scientific purpose only, not for human use.
AZD-3988(AZD3988)|DGAT-1 inhibitor|DC Chemicals
AZD-3988(AZD3988)|DGAT-1 inhibitor|DC Chemicals
AZD-3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM).
Catlog: DC8060| Product name: AZD-3988| Cas: 892489-52-0| Other names: AZD-3988, AZD3988, AZD 3988| Molecule Formula: C23H22F2N4O4| MW: 456.44. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
Potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
For research and scientific purpose only, not for human use.
AZD-3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM).
Catlog: DC8060| Product name: AZD-3988| Cas: 892489-52-0| Other names: AZD-3988, AZD3988, AZD 3988| Molecule Formula: C23H22F2N4O4| MW: 456.44. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
Potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
For research and scientific purpose only, not for human use.
SCD1 inhibitor|cas 1231243-91-6|DC Chemicals
SCD1 inhibitor|cas 1231243-91-6|DC Chemicals
A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
Catlog: DC8069| Product name: SCD1 inhibitor| Cas: 1231243-91-6| Other names: | Molecule Formula: C21H20F3N3O3| MW: 419.14. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
For research and scientific purpose only, not for human use.
A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
Catlog: DC8069| Product name: SCD1 inhibitor| Cas: 1231243-91-6| Other names: | Molecule Formula: C21H20F3N3O3| MW: 419.14. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
For research and scientific purpose only, not for human use.
PF-429242(PF429242)|S1P inhibitor|DC Chemicals
PF-429242(PF429242)|S1P inhibitor|DC Chemicals
PF-429242 is a potent inhibitor of S1P(cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease)
Catlog: DC8059| Product name: PF 429242| Cas: 947303-87-9| Other names: PF-429242,PF429242| Molecule Formula: C25H35N3O2.2HCl| MW: 482.49. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
For research and scientific purpose only, not for human use.
PF-429242 is a potent inhibitor of S1P(cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease)
Catlog: DC8059| Product name: PF 429242| Cas: 947303-87-9| Other names: PF-429242,PF429242| Molecule Formula: C25H35N3O2.2HCl| MW: 482.49. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
For research and scientific purpose only, not for human use.
T-863(T863)|DGAT1 inhibitor|DC Chemicals
T-863(T863)|DGAT1 inhibitor|DC Chemicals
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor
Catlog: DC8058| Product name: T863| Cas: 701232-20-4| Other names: T-863,T 863| Molecule Formula: C22H26N4O3| MW: 394.47. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
For research and scientific purpose only, not for human use.
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor
Catlog: DC8058| Product name: T863| Cas: 701232-20-4| Other names: T-863,T 863| Molecule Formula: C22H26N4O3| MW: 394.47. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
For research and scientific purpose only, not for human use.
(S)-(-)-Etomoxir|828934-43-6|DC Chemicals
(S)-(-)-Etomoxir|828934-43-6|DC Chemicals
S isomer of R-Etomoxir
Catlog: DC8057| Product name: S-Etomxir| Cas: 828934-43-6| Other names: S-Etomoxir,(-)-Etomoxir| Molecule Formula: C15H18ClNaO4| MW: 320.7. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
S isomer of R-Etomoxir
For research and scientific purpose only, not for human use.
S isomer of R-Etomoxir
Catlog: DC8057| Product name: S-Etomxir| Cas: 828934-43-6| Other names: S-Etomoxir,(-)-Etomoxir| Molecule Formula: C15H18ClNaO4| MW: 320.7. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
S isomer of R-Etomoxir
For research and scientific purpose only, not for human use.
(R)-(+)-Etomoxir|CPT1 inhibitor|DC Chemicals
(R)-(+)-Etomoxir|CPT1 inhibitor|DC Chemicals
R-Etomoxir is an inhibitor of carnitine palmitoyltransferase I (CPT1); inhibits β-oxidation in mitochondria.
Catlog: DC8056| Product name: (R)-(+)-Etomoxir| Cas: 828934-41-4| Other names: R-Etomoxir,(+)-Etomoxir| Molecule Formula: C15H18ClNaO4| MW: 320.7. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
R-Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1, the mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver). By regulating fatty acid oxidation, (+)-etomoxir has the potential to affect ketogenesis, cholesterol synthesis, and gluconeogenesis. (+)-Etomoxir has also been identified as a direct agonist of PPARα.
For research and scientific purpose only, not for human use.
R-Etomoxir is an inhibitor of carnitine palmitoyltransferase I (CPT1); inhibits β-oxidation in mitochondria.
Catlog: DC8056| Product name: (R)-(+)-Etomoxir| Cas: 828934-41-4| Other names: R-Etomoxir,(+)-Etomoxir| Molecule Formula: C15H18ClNaO4| MW: 320.7. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
R-Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1, the mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver). By regulating fatty acid oxidation, (+)-etomoxir has the potential to affect ketogenesis, cholesterol synthesis, and gluconeogenesis. (+)-Etomoxir has also been identified as a direct agonist of PPARα.
For research and scientific purpose only, not for human use.
cyclo(-RGDfK)|αvβ3-integrin antagonist|DC Chemicals
cyclo(-RGDfK)|αvβ3-integrin antagonist|DC Chemicals
cyclo(-RGDfK,-Arg-Gly-Asp-D-Phe-Lys)) is a selective αvβ3-integrin antagonist.
Catlog: DC8055| Product name: cyclo(-RGDfK)| Cas: 161552-03-0| Other names: | Molecule Formula: C27H41N9O7| MW: 603.7. Purity: >98%
Price: 100mg: 500 USD; 250mg: 950 USD; 1000mg: 1800 USD
cyclo(-RGDfK,-Arg-Gly-Asp-D-Phe-Lys)) is a selective αvβ3-integrin antagonist. In one study where this peptide was labeled with 125I, it was found to bind specifically and with high affinity to αvβ3 receptors on neovascular blood vessel sections of different major human cancers. The integrin alpha(IIb)beta(3)-specific cyclic hexapeptide contains an Arg-Gly-Asp (RGD) sequence.
For research and scientific purpose only, not for human use.
cyclo(-RGDfK,-Arg-Gly-Asp-D-Phe-Lys)) is a selective αvβ3-integrin antagonist.
Catlog: DC8055| Product name: cyclo(-RGDfK)| Cas: 161552-03-0| Other names: | Molecule Formula: C27H41N9O7| MW: 603.7. Purity: >98%
Price: 100mg: 500 USD; 250mg: 950 USD; 1000mg: 1800 USD
cyclo(-RGDfK,-Arg-Gly-Asp-D-Phe-Lys)) is a selective αvβ3-integrin antagonist. In one study where this peptide was labeled with 125I, it was found to bind specifically and with high affinity to αvβ3 receptors on neovascular blood vessel sections of different major human cancers. The integrin alpha(IIb)beta(3)-specific cyclic hexapeptide contains an Arg-Gly-Asp (RGD) sequence.
For research and scientific purpose only, not for human use.
AZ5104(AZ-5104),metabolite of AZD9291|DC Chemicals
AZ5104(AZ-5104),metabolite of AZD9291|DC Chemicals
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
Catlog: DC8052| Product name: AZ5104| Cas: 1421373-98-9| Other names: AZ-5104,AZ 5104| Molecule Formula: C27H31N7O2| MW: 485.58. Purity: >98%
Price: 100mg: 750 USD; 250mg: 1500 USD; 1000mg: 2600 USD
AZ5104 is an active circulating metabolite of AZD9291. It shares the similar overall activity profile with AZD9219, but is more potent against mutant EGFR forms, while hitting the wild-type EGFR form at a lower concentration thus demonstrating a smaller selectivity margin compared with the parent. Like AZD9291, AZ5104 displays potent antitumor activities both in vitro and in vivo, and is clinically competent with the parent.AZ5104 is a demethylated metabolite of AZD-9291. AZ-5104 was identified to exhibit 5-fold potency compared to AZD-9291, which is currently in clinical trial.
For research and scientific purpose only, not for human use.
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
Catlog: DC8052| Product name: AZ5104| Cas: 1421373-98-9| Other names: AZ-5104,AZ 5104| Molecule Formula: C27H31N7O2| MW: 485.58. Purity: >98%
Price: 100mg: 750 USD; 250mg: 1500 USD; 1000mg: 2600 USD
AZ5104 is an active circulating metabolite of AZD9291. It shares the similar overall activity profile with AZD9219, but is more potent against mutant EGFR forms, while hitting the wild-type EGFR form at a lower concentration thus demonstrating a smaller selectivity margin compared with the parent. Like AZD9291, AZ5104 displays potent antitumor activities both in vitro and in vivo, and is clinically competent with the parent.AZ5104 is a demethylated metabolite of AZD-9291. AZ-5104 was identified to exhibit 5-fold potency compared to AZD-9291, which is currently in clinical trial.
For research and scientific purpose only, not for human use.
AG-120(AG120)|IDH1 inhibitor| Supplied by DC Chemicals
AG-120(AG120)|IDH1 inhibitor| Supplied by DC Chemicals
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
Catlog: DC8051| Product name: AG-120| Cas: 1448347-49-6| Other names: AG120,AG 120| Molecule Formula: C28H22ClF3N6O3| MW: 582.969. Purity: >98%
Price: 100mg: 1200 USD; 250mg: 2400 USD; 1000mg: 3200 USD
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein, and is a highly targeted investigational medicine for the treatment of patients with cancers that harbor an IDH1 mutation. AG-120 specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. IDH1, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
For research and scientific purpose only, not for human use.
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
Catlog: DC8051| Product name: AG-120| Cas: 1448347-49-6| Other names: AG120,AG 120| Molecule Formula: C28H22ClF3N6O3| MW: 582.969. Purity: >98%
Price: 100mg: 1200 USD; 250mg: 2400 USD; 1000mg: 3200 USD
AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein, and is a highly targeted investigational medicine for the treatment of patients with cancers that harbor an IDH1 mutation. AG-120 specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. IDH1, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
For research and scientific purpose only, not for human use.
Akt Inhibitor IV CAS 681281-88-9| DC Chemicals
Akt Inhibitor IV CAS 681281-88-9| DC Chemicals
Akt Inhibitor IV is n Inhibitor of Akt protein kinase
Catlog: DC8050| Product name: Akt Inhibitor IV| Cas: 681281-88-9| Other names: | Molecule Formula: C31H27N4S•I| MW: 614.54. Purity: >98%
Price: 100mg: 950 USD; 250mg: 1800 USD; 1000mg: 3200 USD
Akt Inhibitor IV Inhibits Akt protein kinase. Reports indicate that Akt inhibitor IV targets the ATP-binding site of a kinase upstream of AKT and downstream of PI3K. Akt inhibitor IV was observed to increase the sensitivity of glioma cells to radiaton.
For research and scientific purpose only, not for human use.
Akt Inhibitor IV is n Inhibitor of Akt protein kinase
Catlog: DC8050| Product name: Akt Inhibitor IV| Cas: 681281-88-9| Other names: | Molecule Formula: C31H27N4S•I| MW: 614.54. Purity: >98%
Price: 100mg: 950 USD; 250mg: 1800 USD; 1000mg: 3200 USD
Akt Inhibitor IV Inhibits Akt protein kinase. Reports indicate that Akt inhibitor IV targets the ATP-binding site of a kinase upstream of AKT and downstream of PI3K. Akt inhibitor IV was observed to increase the sensitivity of glioma cells to radiaton.
For research and scientific purpose only, not for human use.
SNG-1153(SNG1153)|ER-α36 modulator|DC Chemicals
SNG-1153(SNG1153)|ER-α36 modulator|DC Chemicals
SNG-1153 is a synthetic modulator of ER-α36
Catlog: DC8049| Product name: SNG-1153| Cas: N/A| Other names: SNG1153,SNG 1153| Molecule Formula: C21H17F305| MW: 406.1. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
SNG1153 is a synthetic ER-α36 modulator, showed promising activities in many in vitro and in vivo models. In-vivo efficacies of SNG1153 were evaluated in Bcap-37 xenograft model, Ishikawa xenograft model and SPC-A-1 xenograft model. Results: SNG1153 showed significant inhibition at low micromolar concentrations in ER-α36 overexpressed cell lines including the one resistant to tamoxifen. SNG1153 exhibited a linear PK profile with a bioavailability of more than 55% in the rat PK study. In the in-vivo efficacy studies, 3 doses were investigated and SNG1153 showed dose-dependent inhibition. The tumor growth inhibition at high dose was 57% in the breast cancer Bcap-37 xenograft model, 65% in the endometrial cancer Ishikawa xenograft model and 52% in lung adenocarcinoma SPC-A-1 xenograft model. No signs of toxicity were observed in these model.
For research and scientific purpose only, not for human use.
SNG-1153 is a synthetic modulator of ER-α36
Catlog: DC8049| Product name: SNG-1153| Cas: N/A| Other names: SNG1153,SNG 1153| Molecule Formula: C21H17F305| MW: 406.1. Purity: >98%
Price: 100mg: 600 USD; 250mg: 1100 USD; 1000mg: 1900 USD
SNG1153 is a synthetic ER-α36 modulator, showed promising activities in many in vitro and in vivo models. In-vivo efficacies of SNG1153 were evaluated in Bcap-37 xenograft model, Ishikawa xenograft model and SPC-A-1 xenograft model. Results: SNG1153 showed significant inhibition at low micromolar concentrations in ER-α36 overexpressed cell lines including the one resistant to tamoxifen. SNG1153 exhibited a linear PK profile with a bioavailability of more than 55% in the rat PK study. In the in-vivo efficacy studies, 3 doses were investigated and SNG1153 showed dose-dependent inhibition. The tumor growth inhibition at high dose was 57% in the breast cancer Bcap-37 xenograft model, 65% in the endometrial cancer Ishikawa xenograft model and 52% in lung adenocarcinoma SPC-A-1 xenograft model. No signs of toxicity were observed in these model.
For research and scientific purpose only, not for human use.
SEP-0372814 cas 1516895-53-6 from DC Chemicals
SEP-0372814 cas 1516895-53-6 from DC Chemicals
Catlog: DC8048| Product name: SEP-0372814| Cas: 1516895-53-6| Other names: SEP 0372814，SEP0372814| Molecule Formula: C21H21N7| MW: 371.19. Purity: >98%
Price: 100mg: 1300 USD; 250mg: 2200 USD; 1000mg: 4000 USD
For research and scientific purpose only, not for human use.
Catlog: DC8048| Product name: SEP-0372814| Cas: 1516895-53-6| Other names: SEP 0372814，SEP0372814| Molecule Formula: C21H21N7| MW: 371.19. Purity: >98%
Price: 100mg: 1300 USD; 250mg: 2200 USD; 1000mg: 4000 USD
For research and scientific purpose only, not for human use.
VRT-1353385|cas 1616113-45-1|DC Chemicals
VRT-1353385|cas 1616113-45-1|DC Chemicals
Catlog: DC8047| Product name: VRT-1353385| Cas: 1616113-45-1| Other names: VRT 1353385,VRT1353385| Molecule Formula: C36H41NO10| MW: 647.71. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
For research and scientific purpose only, not for human use.
Catlog: DC8047| Product name: VRT-1353385| Cas: 1616113-45-1| Other names: VRT 1353385,VRT1353385| Molecule Formula: C36H41NO10| MW: 647.71. Purity: >98%
Price: 100mg: 800 USD; 250mg: 1500 USD; 1000mg: 2800 USD
For research and scientific purpose only, not for human use.
BIO-32546|CAS 1548743-66-3| DC Chemicals
BIO-32546|CAS 1548743-66-3| DC Chemicals
Catlog: DC8046| Product name: BIO-32546| Cas: 1548743-66-3| Other names: BIO 32546,BIO32546| Molecule Formula: C28H31F6NO3| MW: 543.54. Purity: >98%
Price: 100mg: 2000 USD; 250mg: 3500 USD; 1000mg: 6000 USD
For research and scientific purpose only, not for human use.
Catlog: DC8046| Product name: BIO-32546| Cas: 1548743-66-3| Other names: BIO 32546,BIO32546| Molecule Formula: C28H31F6NO3| MW: 543.54. Purity: >98%
Price: 100mg: 2000 USD; 250mg: 3500 USD; 1000mg: 6000 USD
For research and scientific purpose only, not for human use.
Tie-2 inhibitor 7|cas 1020412-97-8|DC Chemicals
Tie-2 inhibitor 7|cas 1020412-97-8|DC Chemicals
An agent that inhibits endothelial cell tube formation
Catlog: DC8045| Product name: Tie-2 inhibitor 7| Cas: 1020412-97-8| Other names: Tie2 inhibitor,Tie inhibitor 7| Molecule Formula: C31H29N3O5| MW: 523.6. Purity: >98%
Price: 10mg: 400 USD; 250mg: 800 USD; 1000mg: 1600 USD
Tie-2 Inhibitor 7 can permeate the cell (IC50= 1μM) and inhibit endothelial cell tube formation. Research shows that it can block the Tie-2 ligand, Ang-1 (angiopoietin), which induces Tie-2 autophosphorylation and block its downstream signaling with an IC50= 0.3 μM. Vascular leakage, suppression of endothelial apoptosis, and vessel regression are strongly inhibited by Ang-1. The Tie-2 receptor plays a crucial role in the normal and pathologic vascular development of epithelial cells.
For research and scientific purpose only, not for human use.
An agent that inhibits endothelial cell tube formation
Catlog: DC8045| Product name: Tie-2 inhibitor 7| Cas: 1020412-97-8| Other names: Tie2 inhibitor,Tie inhibitor 7| Molecule Formula: C31H29N3O5| MW: 523.6. Purity: >98%
Price: 10mg: 400 USD; 250mg: 800 USD; 1000mg: 1600 USD
Tie-2 Inhibitor 7 can permeate the cell (IC50= 1μM) and inhibit endothelial cell tube formation. Research shows that it can block the Tie-2 ligand, Ang-1 (angiopoietin), which induces Tie-2 autophosphorylation and block its downstream signaling with an IC50= 0.3 μM. Vascular leakage, suppression of endothelial apoptosis, and vessel regression are strongly inhibited by Ang-1. The Tie-2 receptor plays a crucial role in the normal and pathologic vascular development of epithelial cells.
For research and scientific purpose only, not for human use.
GSK-503|GSK503|EZH2 inhibitor|DC CHEMICALS
GSK-503|GSK503|EZH2 inhibitor|DC CHEMICALS
GSK503 is a specific EZH2 methyltransferase inhibitor.
Catlog: DC8044| Product name: GSK-503| Cas: 1346572-63-1| Other names: GSK-503,GSK503,GSK 503| Molecule Formula: C31H38N6O2| MW: 526.3. Purity: >98%
Price: 100mg: 950 USD; 250mg: 1800 USD; 1000mg: 3000 USD
GSK503 is a specific EZH2 methyltransferase inhibitor or vehicle. GSK503 was designed by performing high-throughput screening for EZH2 methyltransferase inhibiting compounds followed by chemical optimization.GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Kappi=3−27nM) and is structurally related to GSK126 and GSK343. GSK503 was > 200 fold selective over EZH1 (Kappi=636nM) and > 4000 fold selective over other histone methyltransferases. GSK503 displayed favorable pharmacokinetics in mice and was thus selected for use in in vivo experiments.
For research and scientific purpose only, not for human use.
GSK503 is a specific EZH2 methyltransferase inhibitor.
Catlog: DC8044| Product name: GSK-503| Cas: 1346572-63-1| Other names: GSK-503,GSK503,GSK 503| Molecule Formula: C31H38N6O2| MW: 526.3. Purity: >98%
Price: 100mg: 950 USD; 250mg: 1800 USD; 1000mg: 3000 USD
GSK503 is a specific EZH2 methyltransferase inhibitor or vehicle. GSK503 was designed by performing high-throughput screening for EZH2 methyltransferase inhibiting compounds followed by chemical optimization.GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Kappi=3−27nM) and is structurally related to GSK126 and GSK343. GSK503 was > 200 fold selective over EZH1 (Kappi=636nM) and > 4000 fold selective over other histone methyltransferases. GSK503 displayed favorable pharmacokinetics in mice and was thus selected for use in in vivo experiments.
For research and scientific purpose only, not for human use.
OTS-514,OTS514|TOPK inhibitor|DC Chemicals
OTS-514,OTS514|TOPK inhibitor|DC Chemicals
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor. IC50:2.6nM
Catlog: DC8043| Product name: OTS514|Price: 100mg: 1200 USD; 250mg: 2200 USD; 1000mg: 4200 USD
Cas: N/A| Other names: OTS514,OTS 514,OTS-514| Molecule Formula: C21H20N2O2S| MW: 364. Purity: >98%
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor,IC50:2.6nM. The compound can inhibit TOPK kinase activity. TOPK (T-lymphokine-activated killer cell-originated protein kinase) is a protein that is found in a wide range of human cancers and is believed to work as an oncogene, promoting tumor growth.The enzyme shows highly elevated expression in several cancers including lymphomas, breast cancer and lung cancer. Its activity peaks in the M phase of the cell-division cycle, during which it phosphorylates several proteins involved in cancer cell cytokinesis, such as histone H3, protein regulator of cytokinesis 1 (PRC1), G protein signaling modulator 2 (GPSM2) and valosin containing protein.Many cancer cells upregulate TOPK and require its activity to drive their rapidly progressing cell cycles. Because the kinase is either not expressed or expressed at relatively low levels in most healthy tissues, targeting it in cancer cells could eliminate some of the risks associated with other cytokinesis enzymes.
It has been reported that OTS514 strongly inhibited the growth of the TOPK-positive cancer cell lines with low IC50 values ranging from 1.5 to 14 nM. While in HT29 cells, in which TOPK expression was little detectable, the IC50 value was 170 nM. Intravenous administration of free OTS514 at 1, 2.5, and 5mg/kg once a day for 2 weeks resulted in tumor growth Inhibition（TGI）of 5.7, 43.3, and 65.3% on day 15, respectively, without anybody weight loss. However, this inhibition also cause dysfunction in the differentiation process of hematopoietic stemcells (HSCs) to WBCs and RBCs but may enhance the differentiation of HSCs to megakaryocytes and platelets.
The antitumor effect of OTS514 in lung cancer xenograft model of LU-99 cells has also been investigated. OTS514 was administered to mice bearing LU-99 cancer cells after the tumor size reached about 200mm3. Intravenous administration of OTS514 (5 mg/kg) once a day for 2 weeks achieved good growth-suppressive effect with TGI of 104% without any body weight loss. However, the antitumor effect of OTS514 against LU-99 xenograft caused a significant reduction of WBCs.
For the detailed information of OTS514, the solubility of OTS514 in water, the solubility of OTS514 in DMSO, the solubility of OTS514 in PBS buffer, the animal experiment (test) of OTS514, the cell expriment (test) of OTS514, the in vivo, in vitro and clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514, For the detailed information of OTS514, the solubility of OTS514 in water, the solubility of OTS514 in DMSO, the solubility of OTS514 in PBS buffer, the animal experiment (test) of OTS514, the cell expriment (test) of OTS514, the in vivo, in vitro and clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514, Please contact DC Chemicals.
For research and scientific purpose only, not for human use.
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor. IC50:2.6nM
Catlog: DC8043| Product name: OTS514|Price: 100mg: 1200 USD; 250mg: 2200 USD; 1000mg: 4200 USD
Cas: N/A| Other names: OTS514,OTS 514,OTS-514| Molecule Formula: C21H20N2O2S| MW: 364. Purity: >98%
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor,IC50:2.6nM. The compound can inhibit TOPK kinase activity. TOPK (T-lymphokine-activated killer cell-originated protein kinase) is a protein that is found in a wide range of human cancers and is believed to work as an oncogene, promoting tumor growth.The enzyme shows highly elevated expression in several cancers including lymphomas, breast cancer and lung cancer. Its activity peaks in the M phase of the cell-division cycle, during which it phosphorylates several proteins involved in cancer cell cytokinesis, such as histone H3, protein regulator of cytokinesis 1 (PRC1), G protein signaling modulator 2 (GPSM2) and valosin containing protein.Many cancer cells upregulate TOPK and require its activity to drive their rapidly progressing cell cycles. Because the kinase is either not expressed or expressed at relatively low levels in most healthy tissues, targeting it in cancer cells could eliminate some of the risks associated with other cytokinesis enzymes.
It has been reported that OTS514 strongly inhibited the growth of the TOPK-positive cancer cell lines with low IC50 values ranging from 1.5 to 14 nM. While in HT29 cells, in which TOPK expression was little detectable, the IC50 value was 170 nM. Intravenous administration of free OTS514 at 1, 2.5, and 5mg/kg once a day for 2 weeks resulted in tumor growth Inhibition（TGI）of 5.7, 43.3, and 65.3% on day 15, respectively, without anybody weight loss. However, this inhibition also cause dysfunction in the differentiation process of hematopoietic stemcells (HSCs) to WBCs and RBCs but may enhance the differentiation of HSCs to megakaryocytes and platelets.
The antitumor effect of OTS514 in lung cancer xenograft model of LU-99 cells has also been investigated. OTS514 was administered to mice bearing LU-99 cancer cells after the tumor size reached about 200mm3. Intravenous administration of OTS514 (5 mg/kg) once a day for 2 weeks achieved good growth-suppressive effect with TGI of 104% without any body weight loss. However, the antitumor effect of OTS514 against LU-99 xenograft caused a significant reduction of WBCs.
For the detailed information of OTS514, the solubility of OTS514 in water, the solubility of OTS514 in DMSO, the solubility of OTS514 in PBS buffer, the animal experiment (test) of OTS514, the cell expriment (test) of OTS514, the in vivo, in vitro and clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514, For the detailed information of OTS514, the solubility of OTS514 in water, the solubility of OTS514 in DMSO, the solubility of OTS514 in PBS buffer, the animal experiment (test) of OTS514, the cell expriment (test) of OTS514, the in vivo, in vitro and clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514, Please contact DC Chemicals.
For research and scientific purpose only, not for human use.
2015年5月25日星期一
stem cell related compounds from DC Chemicasl
DC Chemicals focus to develop Stem Cell related compounds.
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Stem cell
Compounds
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Cas No.
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Promoting
Pricing
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1
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CHIR99021
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252917-06-9
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price:
1600 USD/gram, 8000 USD/10grams. In stock.
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Highly
selective GSK-3 inhibitor; enables reprogramming of mouse embryonic
fibroblasts into iPS cells
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purity>98%
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2
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Y-27632 2HCL
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129830-38-2
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Price: 1700 USD/gram,
9000 USD/10grams, more than 30 grams in stock.
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Selective
p160ROCK inhibitor; increases survival rate of human embryonic stem cells
undergoing cryopreservation
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purity>99.5%
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3
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Thiazovivin
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1226056-71-8
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1300 USD/gram,
7500 USD/10grams. More than 35 grams In stock.
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Improves the
efficiency of fibroblast reprogramming and induction of iPSCs
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purity>98%
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4
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PD-0325901
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391210-10-9
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price:
1200 USD/gram, 6000 USD/10grams. More than 40 grams In stock.
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Selective
inhibitor of MEK1/2; enhances generation of iPSCs
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purity>99%,
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5
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A83-01
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price: 1800
USD/gram, 9500 USD/10grams. In stock.
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Selective
inhibitor of TGF-βRI, ALK4 and ALK7; maintains self-renewal of human iPSCs
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purity>98%
(By HNMR)
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6
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SB-431542
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301836-41-9
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price: 1200
USD/gram, 6000 USD/10grams. 15 grams In stock.
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Potent,
selective inhibitor of TGF-βRI, ALK4 and ALK7
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purity>99%,
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||
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7
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CASIN
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425399-05-9
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1300 USD/gram,
7500 USD/10grams. In stock
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Cdc42 GTPase
inhibitor; functionally rejuvenates aged HSCs
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purity>98%
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8
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Dorsomorphin 2HCl
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Price: 1700
USD/gram, 9000 USD/10grams, more than 20 grams in stock.
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|
|
a potent inhibitor of AMP-activated protein
kinase (AMPK) (Ki=109nM) and bone morphogenic protein (BMP) signaling
|
purity>98%
|
||
|
9
|
LDN-193189
|
1062368-24-4
|
price: 1800
USD/gram, 9500 USD/10grams. In stock.
|
|
BMP pathway
inhibitor Inhibits ALK2, ALK3, ALK6
|
purity>98%
|
||
|
10
|
StemRegenin 1
(SR1)
|
1227633-49-9
|
1200 USD/gram
4500 USD/5grams，7000 USD/10 grams, In stock
|
|
Aryl
hydrocarbon receptor (AhR) antagonist
|
purity>98%
|
||
|
11
|
A77-01
|
||
|
An inhibitor
of ALK5 with an IC50 of 25nM
|
|||
|
12
|
CHIR98014
|
252935-94-7
|
price: 1800
USD/gram, 9500 USD/10grams. 6 grams In stock.
|
|
A selective
and ATP-competitive inhibitor of GSK-3β,higher activity than CHIR99021
|
purity>99%,
|
||
|
13
|
BIO
|
667463-62-9
|
price:
1800 USD/gram,9000 USD/10grams. 10 grams In stock.
|
|
Potent,
selective GSK-3 inhibitor
|
purity>98%
|
||
|
14
|
GDC-0449
|
879085-55-9
|
price: 1200
USD/gram, 6000 USD/10grams
|
|
GDC 0449 is a
potent antagonist of SMO that acts in a biphasic manner
|
Purity>98%
|
||
|
15
|
NVP-LDE225
|
956697-53-3
|
price: 1300
USD/gram,6500 USD/10grams. In stock.
|
|
A novel and
specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM.
|
purity>99%,
|
||
|
16
|
Repsox (ALK5
INHIBITOR)
|
446859-33-2
|
price: 1200
USD/gram, 6500 USD/10grams. More than 20 grams In stock.
|
|
Selective
TGF-βRI inhibitor; enhances reprogramming efficiency
|
purity>98%
|
||
|
17
|
XAV-939
|
284028-89-3
|
price: 1200
USD/gram, 6500 USD/10grams. More than 20 grams In stock.
|
|
Tankyrase
inhibitor; promotes cardiomyogenesis
|
purity>99%
|
||
|
18
|
DAPT
|
208255-80-5
|
price: 1000
USD/gram, 5500 USD/10grams. More than 15 grams In stock.
|
|
A
gamma-secretase and indirectly Notch, LDL receptor-related protein,
E-cadherin and ErbB-4 inhibitor.
|
purity>98%
|
||
|
19
|
GDC-0941
|
957054-30-7
|
price: 1200
USD/gram, 6000 USD/10grams, In stock
|
|
Anovel class I
selective PI3K inhibitor
|
purity>98%
|
||
|
20
|
LY-294002
|
154447-36-6,
|
price: 1200
USD/gram, 6000 USD/10grams.More than 20 grams In stock.
|
|
Selective PI 3-kinase
inhibitor; suppresses proliferation of mESCs
|
purity>99%
|
||
|
21
|
KY02111
|
1118807-13-8
|
price: 1200
USD/gram, 6000 USD/10grams.In stock.
|
|
Promotes
differentiation of human ESCs and iPSCs into cardiomyocytes when used after
day three in culture
|
Purity>98%
|
||
|
22
|
IWR-1-endo
|
1127442-82-3
|
price: 1200
USD/gram, 6000 USD/10grams. In stock.
|
|
Axin
stabilizer; promotes β-catenin phosphorylation
|
Purity>99%
|
||
|
23
|
IWP-2
|
686770-61-6
|
1800 USD/gram,
9000 USD/10grams. In stock.
|
|
Inhibitor of
Wnt processing and secretion; suppresses self-renewal in R1 ESCs
|
purity>98%
|
||
|
25
|
GANT-61
|
500579-04-4
|
price: 1200
USD/gram, 6000 USD/10grams. In stock.
|
|
GLI
antagonist; inhibits Hh signaling
|
Purity>98%
|
||
|
26
|
SB-203580
|
152121-47-6
|
price: 1200
USD/gram, 6000 USD/10grams. In stock.
|
|
Selective
inhibitor of p38 MAPK; stimulates neural stem cell proliferation
|
Purity>99%
|
||
|
27
|
BIX 01294
|
935693-62-2
|
1300 USD/gram,
9500 USD/10grams, In stock
|
|
G9a-like
protein and G9a HMTase inhibitor; potentiates induction of iPSCs
|
purity:>98%
|
||
|
28
|
JW 55
|
664993-53-7
|
1300 USD/gram,
8000 USD/10grams, In stock
|
|
Inhibitor of
the PARP domain of tankyrase 1 and 2 (TNKS1/2)
|
purity:>98%
|
||
|
29
|
PluriSIn 1 (NSC
14613)
|
91396-88-2
|
1200
USD/gram, 8000 USD/10grams, In stock
|
|
Inhibitor of
SCD1; selectively eliminates undifferentiated hPSCs from culture
|
purity:>98%
|
||
|
30
|
Purmorphamine
|
483367-10-8
|
1600 USD/gram,
9500 USD/10grams, In stock
|
|
Smo receptor
agonist; induces differentiation of mesenchymal progenitor cells into
osteoblasts
|
purity:>98%
|
||
|
31
|
AR-A014418
|
487021-52-3,
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
Selective
glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM).
|
purity>98%
|
||
|
32
|
A 769662
|
844499-71-4
|
1200 USD/gram,
6000 USD/10grams , In stock
|
|
Potent AMPK
activator; inhibits MSC proliferation
|
purity:>98%
|
||
|
33
|
GW788388
|
452342-67-5
|
1200
USD/gram, 8000 USD/10grams, In stock
|
|
Potent
inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values
are 18 and 93 nM for ALK5 binding and for TGF-β cellular assay respectively).
|
purity>98%
|
||
|
34
|
Forskolin
|
66575-29-9
|
1500 USD/gram,
8000 USD/10grams, In stock
|
|
Used to
reprogram mouse embryonic fibroblasts to induced pluripotent stem cells
|
purity>98%
|
||
|
35
|
P7C3
|
301353-96-8
|
1200
USD/gram, 8000 USD/10grams, In stock
|
|
Neuroprotective
compound; enhances neurogenesis in vivo
|
purity:>98%
|
||
|
36
|
MK-2206 2HCl
|
1032350-13-2
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
AnAkt
inhibitor
|
purity:>98%
|
||
|
37
|
ID-8
|
147591-46-6
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
Sustains self-renewal
and pluripotency of ESCs
|
purity:>98%
|
||
|
38
|
FH1(BRD-K4477)
|
CAS 2719-05-3
|
1200
USD/gram, 8000 USD/10grams, In stock
|
|
Enhances
differentiation of induced pluripotent stem cells (iPSCs) to hepatocytes and
promotes the maturation of iPSC-derived hepatocytes.
|
purity:>98%
|
||
|
39
|
Reversine
|
656820-32-5
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
The first
organic molecule that has been demonstrated to reverse the cellular
differentiation process.
|
purity:>98%
|
||
|
40
|
RG-108
|
48208-26-0
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
Non-nucleoside
DNA methyltransferase inhibitor; enhances efficiency of iPSC generation
|
purity:>98%
|
||
|
41
|
Wnt-C59
|
1243243-89-1
|
1200 USD/gram,
7000 USD/10 grams, In stock
|
|
Wnt signaling
inhibitor; induces differentiation of iPSCs to cardiomyocytes
|
purity:>98%
|
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