2018年5月18日星期五

SAGE-217|SAGE217|cas 1632051-40-1

SAGE-217|SAGE217|cas 1632051-40-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: SAGE-217|CAS: 1632051-40-1|Cat No: DC10802|Other Names: SAGE-217; SAGE 217; SAGE217,1632051-40-1

SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.

Kinase assay demonstrates that SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. SAGE-217 is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD) and major depressive disorder (MDD). SAGE-217 shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentration of SAGE-217, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) is noted.Acute administration of SAGE-217 (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) as well as produces a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat lithium-pilocarpine model of status epilepticus (SE), SAGE-217 (0.3 to 5 mg, iv) abolishes both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Additional PK studies of SAGE-217 in dog show low clearance (<10% of hepatic blood flow), resulting in excellent oral bioavailability (F=68%).

AMPA/kainate antagonist-2

AMPA/kainate antagonist-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: AMPA/kainate antagonist-2|CAS: 923271-87-8|Cat No: DC10801|Other Names:

A novel Non-competitive AMPA/kainate antagonist.


AMPA/kainate antagonist-1

AMPA/kainate antagonist-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: AMPA/kainate antagonist-1|CAS: 732277-05-3|Cat No: DC10800|Other Names:

A novel Non-competitive AMPA/kainate antagonist.


D-Lin-MC3-DMA|for siRNA delivery|Supplier

D-Lin-MC3-DMA|for siRNA delivery|Supplier

DC Chemicals, Website:www.dcchemicals.com

Product Name: DLin-MC3-DMA|CAS: N/A|Cat No: DC10800|Other Names: D-Lin-MC3-DMA,DLinMC3DMA,D-Lin-MC-3-DMA,D-Lin-MC3-DMA

D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.

Technological advances in both siRNA (small interfering RNA) and whole genome sequencing have demonstrated great potential in translating genetic information into siRNA-based drugs to halt the synthesis of most disease-causing proteins. Despite its powerful promises as a drug, siRNA requires a sophisticated delivery vehicle because of its rapid degradation in the circulation, inefficient accumulation in target tissues and inability to cross cell membranes to access the cytoplasm where it functions. Lipid nanoparticle (LNP) containing ionizable amino lipids is the leading delivery technology for siRNA, with five products in clinical trials and more in the pipeline.  Lipid nanoparticles (LNPs) formed by an ionizable cationic lipid (DLin-MC3-DMA), helper lipids (distearoylphosphatidylcholine, DSPC, and cholesterol), and a poly(ethylene glycol) (PEG) lipid have been identified as very promising delivery vectors of short interfering RNA (siRNA) in different clinical phases. DLin-MC3-DMA [14], which are 100-fold and 1000-fold more potent, respectively, in silencing of a hepatic gene (Factor VII) in comparison to the previous generation lipid DLin-DMA (1,2-dilinoleyloxy-N,N-dimethyl-3-aminopropane).The ED50 (median effective dose) for LNP containing DLin-MC3-DMA to silence Factor VII in mice and TTR in non-human primates was 0.005 mg/kg and 0.03 mg/kg, respectively. One of the key findings from these studies was the optimum lipid pKa value of 6.2–6.5 as a dominating factor in determining hepatic gene-silencing activity in vivo. DLin-MC3-DMA, having a pKa of 6.44, is currently the most active ionizable lipid being used in clinical trials.

SSR-240612|SSR240612|cas 464930-42-5

SSR-240612|SSR240612|cas 464930-42-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: SSR-240612 HCl |CAS: 464930-42-5|Cat No: DC10799|Other Names: SSR-240612; SSR240612; SSR 240612

SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.

SSR240612 blocked tactile and cold allodynia at 3h (ID50=5.5and 7.1mg/kg,respectively) in glucose‐fed rats but had no effect in control rats. The antagonist (10mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats.

p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3

p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: p38-α MAPK-IN-1|CAS: 443913-15-3|Cat No: DC10798|Other Names: MAPK14 inhibitor

p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor

AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: AB423|CAS: 1572510-80-5|Cat No: DC10797|Other Names: AB423,AB-423,AB 423

AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.

AB-423 is a potent, highly seletive inhibitor of HBV replication through a block of pgRNA encapsidation. AB-423 in combination with EVT has shown synergistic antiviral activity in vitro in primary human hepatocytes. Furthermore, AB-423 alone and in combination with entecavir has shown potent in vivo activity in a hydrodynamic injection (HDI) mouse model of HBV.The HBV capsid inhibitor AB-423 exhibits a dual mode of inhibition:inhibited encapsidation of pgRNA during ongoing infection; inhibited cccDNA synthesis presumably via inhibition of the capsid uncoating step.In vitro AB-423 showed: pan-genotypic activity; potent activity against HBV in combination with Nucs, IFN, and RNAi agents;no significant activity against unrelated viruses.

Prexasertib (LY2606368)|LY 2606368|DC Chemicals

Prexasertib (LY2606368)|LY 2606368|DC Chemicals

DC Chemicals, Website:www.dcchemicals.com

Product Name: Prexasertib (LY2606368) |CAS: 1234015-52-1|Cat No: DC10796|Other Names: LY 2606368,LY-2606368

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.LY2606368 alone significantly inhibited the cell proliferation in a variety of pancreatic cell lines (SW1990, SU86.86, Bx-PC3, AsPC-1, CFPAC-1, Capan-2, HPAF-II) with SW1990 being the most sensitive (IC50=1.5 nM).
LY2606368 has been reported to inhibit Chk1 auto-phosphorylation activated by DNA damaging agents, and induce phosphorylation of H2AX, a DNA damage maker in multiple cancer cell lines in vitro. In addition, LY2606368 has demonstrated potent single agent activity and potentiates the anti-tumor activity of DNA damaging agents in vivo. Pancreatic cancer is one of the least curable cancers, with an approximate 5% overall 5-year survival for all patients. In SW1990 pancreas orthotopic model, which represents the local and metastatic growth pattern seen in pancreas cancer patients, LY2606368 treatment resulted in over 92% inhibition of primary tumor growth as well as 100% inhibition of metastasis to lymph node, spleen and intestine. The anti-tumor effect of LY2606368 treatment was further demonstrated in comparing with gemcitabine (the standard of care for pancreas cancer patient) in SW1990 orthotopic model. For the detailed information of LY2606368 dihydrochloride, the solubility of LY2606368 dihydrochloride in water, the solubility of LY2606368 dihydrochloride in DMSO, the solubility of LY2606368 dihydrochloride in PBS buffer, the animal experiment (test) of  LY2606368 dihydrochloride, the cell expriment (test) of LY2606368 dihydrochloride, the in vivo, in vitro and clinical trial test of LY2606368 dihydrochloride, the EC50, IC50,and affinity,of LY2606368 dihydrochloride, Please contact DC Chemicals.

CM-272|CM272|CAS 1846570-31-7

CM-272|CM272|CAS 1846570-31-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: CM-272|CAS: 1846570-31-7|Cat No: DC10795|Other Names: CM-272; CM 272; CM272

CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies.

CM-272 is a first-in-class reversible and substrate-competitive dual inhibitor of G9a and DNMTs. In ALL, AML and DLBCL-derived cell lines, CM-272 reduced DNA methylation in the promoter region of specific tumor suppressor genes. CM-272 also inhibited cell proliferation, blocked cell cycle progression and induced apoptosis in a dose-dependent way.

PH-002,PH002|AD treament|apo E4 inhibitor

PH-002,PH002|AD treament|apo E4 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: PH-002|CAS: 1311174-68-1|Cat No: DC10794|Other Names: PH002,PH-002,PH 002


PH-002 is a small-molecule structure corrector,inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction,a potent candidate drug for the treament of AD(Alzheimer disease)


PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that restores mitochondrial cytochrome c oxidase subunit 1 levels, rescues impairments of mitochondrial motility and neurite outgrowth. PH-002 is an apoE4 structure corrector that reverses the apoE4 detrimental effects. The researchers confirmed that, in human neurons, the misshapen apoE4 protein cannot function properly and is broken down into disease-causing fragments in the cells. This process results in a number of problems commonly found in Alzheimer's disease, including the accumulation of the protein tau and of amyloid peptides.

ML 221|ML221|CAS 877636-42-5

ML 221|ML221|CAS 877636-42-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: ML221|CAS: 877636-42-5|Cat No: DC10793|Other Names: ML221; ML 221; ML-221

ML221 is an antagonist of the apelin (APJ) receptor.

Apelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.

DIM-C-pPhOCH3(C-DIM5)|Nur77 antagonist|CAS 151358-47-3

DIM-C-pPhOCH3(C-DIM5)|Nur77 antagonist|CAS 151358-47-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: DIM-C-pPhOCH3(C-DIM5)|CAS: 33985-68-1|Cat No: DC10792|Other Names:

C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival,

C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival, induction of apoptosis, induced expression of the apoptosis gene/protein TRAIL, and inhibited tumor growth in vivo. C-DIM5 induces G0-G1–phase to S-phase arrest in Panc1 cells, and this is accompanied by Nur77-dependent induction of the cyclin-dependent kinase inhibitor p21.

DIM-C-pPhOH(CDIM8)|Nur77 antagonist|CAS 151358-47-3

DIM-C-pPhOH(CDIM8)|Nur77 antagonist|CAS 151358-47-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: DIM-C-pPhOH(CDIM8)|CAS: 151358-47-3|Cat No: DC10791|Other Names:

DIM-C-pPhOH is a Nur77 Antagonist. DIM-C-pPhOH inhibits lung cancer cell and tumor growth in a metastasis model.

Nur77 (NR4A1) antagonist. Inhibits TGF-β induced cell migration of breast cancer cell lines. Promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines. Mimics effects of Nur77 RNAi silencing.

ML-239|ML239|CAS 1378872-36-6

ML-239|ML239|CAS 1378872-36-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: ML-239|CAS: 1378872-36-6|Cat No: DC10790|Other Names: CID-49843203,CID 49843203,CID49843203,ML-239,ML 239,ML239,1378872-36-6

ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).

ML239 (Compound 7j) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM, with ∼24-fold selectivity against the control cell line. ML239 inhibits breast cancer stem-like cells, most likely through activation of fatty acid desaturase 2 (FADS2). ML239 is cytotoxic to NCIH661 cells, and FADS2 knockdown reduces ML239 cytotoxicity, and furthermore, FADS2 inhibitor SC-26196 also reduces ML239 cytotoxicity in cancer cell lines (CCLs).

AZD7545|AZD-7545|cas 1816294-67-3

AZD7545|AZD-7545|cas 1816294-67-3 

DC Chemicals, Website:www.dcchemicals.com

Product Name: AZD7545|CAS: 1816294-67-3|Cat No: DC10789|Other Names: AZD7545,AZD-7545,AZD 7545

AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.

AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively. IC50 Value: 36.8 nM (PDHK1); 6.4 nM (PDHK2) [1] Target: PDHK1/2 in vitro: The IC50 values for inhibition of PDHK2 and PDHK1 by AZD7545 were 6.4 ± 2.2 nM (n = 6) and 36.8 ± 18 nM (n = 3) respectively. Other compounds in this series inhibited both PDHK1 and PDHK2 and a consistent trend of reduced potency (5-15-fold) towards PDHK1, as compared with PDHK2, was observed. In contrast, AZD7545 and related compounds failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity [1]. In the presence of PDHK2, AZD7545 increased PDH activity with an EC(50) value of 5.2 nM. In rat hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2]. in vivo: A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. Obese, insulin-resistant, Zucker rats show elevated postprandial glucose levels compared with their lean counterparts (8.7 versus 6.1 mM at 12 weeks old). AZD7545 (10 mg/kg) twice daily for 7 days markedly improved the 24-h glucose profile, by eliminating the postprandial elevation in blood glucose [2]. An interesting observation is that administration of maximally effective doses of AZD7545 and related compounds to rats results in the near-complete activation of PDH activity in liver, where PDHK2 is the major isoenzyme, while only partial activation of PDH activity is achieved in skeletal muscle and heart, tissues which express high levels of PDHK4. For example, following administration of a maximally effective dose of compound K (30 mg/kg) the percentage of PDH present in the active (dephosphorylated) state in liver is elevated from 35.3 ± 4.0% to 90.2 ± 2.2% while in skeletal muscle and heart PDH activity plateaus at 64.3 ± 2.3% and 61.8 ± 4.3% respectively. Further evidence for a link between in vitro isoenzyme selectivity and in vivo activity comes from the observation that in fasted rats the ability of AZD7545 to elevate PDH activity in liver is intact, while the activation of skeletal muscle PDH activity in response to the compound is severely blunted.

SR-4370|SR4370|HDAC inhibitor|CAS 1816294-67-3

SR-4370|SR4370|HDAC inhibitor|CAS 1816294-67-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: SR-4370|CAS: 1816294-67-3 |Cat No: DC10788|Other Names: SR-4370; SR 4370; SR4370

SR-​4370 is an HDAC inhibitor. SR-​4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp.


GSK2982772|GSK-2982772|RIP1 inhibitor

GSK2982772|GSK-2982772|RIP1 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: GSK2982772|CAS: 1622848-92-3|Cat No: DC10787|Other Names: GSK 2982772,GSK-2982772,GSK2982772,1622848-92-3

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.


PLX51107|PLX-51107|BRD4 inhibitor

PLX51107|PLX-51107|BRD4 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: PLX51107|CAS: 1627929-55-8|Cat No: DC10786|Other Names: PLX51107,PLX 51107,PLX-51107

PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.


MK-7246|MK7246|cas 1218918-62-7

MK-7246|MK7246|cas 1218918-62-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: MK-7246|CAS: 1218918-62-7|Cat No: DC10785|Other Names: MK7246,MK 7246,MK-7246

MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.

The affinity and selectivity of MK-7246 for human CRTH2 and recombinant human prostanoid receptors is determined by equilibrium competition analysis using the relevant radioligands and cell membranes expressing the various receptors. MK-7246 competes for [3H]PGD2 specific binding to cell membranes expressing recombinant human CRTH2 with high-affinity (Ki, 2.5 nM). MK-7246 displays a relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (Ki, 373±96 nM) and ≥1500-fold lower for the other prostanoid receptors (Ki, 7668±2169 nM for EP2, 3804±1290 nM for TP). MK-7246 is also tested in a panel of 157 enzyme and receptor assays at concentrations up to 100 μM and small but significant activity is detected only on phosphodiesterase 1 (PDE1, IC50=33.2 μM) and MAPK3 (ERK1, IC50=49.4 μM).Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). Mast cell derived production of Prostaglandin D2 (PGD2) is believed to be a prime mediator of allergic inflammation. Since CRTH2 plays an important role in the early aspects of the allergic inflammation cascade, the effect of the CRTH2 antagonist is examined on A. alternate elicited pulmonary inflammatory responses. CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05).

E7820|E-7820|cas 289483-69-8

E7820|E-7820|cas 289483-69-8

DC Chemicals, Website:www.dcchemicals.com

Product Name: E7820|CAS: 289483-69-8|Cat No: DC10784|Other Names: ER68203-00,E7820,E-7820,E 7820,289483-69-8

E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.

E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50 values are 0.20 and 0.24 μg/mL, respectively.E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.

PF-9366|PF9366|cas 72882-78-1

PF-9366|PF9366|cas 72882-78-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: PF-9366|CAS: 72882-78-1|Cat No: DC10783|Other Names: PF-9366; PF 9366; PF9366,72882-78-1

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.

PF-9366 is a Mat2A inhibitor, with an IC50 of 420 nM and a Kd of 170 nM. PF-9366 displays no substantial off-target activity in GPCRs, neurotransporters, phosphodiesterases, and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibits cellular S-Adenosyl-L-methionine (SAM) production with an IC50 of 1.2 μM in H520 lung carcinoma cells. PF-9366 is more potent in Huh-7 cells against SAM synthesis, with an IC50 of 255 nM, and also suppresses the proliferation of cells with an IC50 of 10 μM.


LY2510924|LY-2510924|CXCR4 inhibitor

LY2510924|LY-2510924|CXCR4 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: LY2510924|CAS: 1088715-84-7 |Cat No: DC10782|Other Names: LY2510924; LY-2510924; LY 2510924

LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity.

LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity. Upon subcutaneous administration, CXCR4 inhibitor LY2510924 binds to the chemokine receptor CXCR4, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor activation. This may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types.

ASK-IN-1|cas 1262041-49-5

ASK-IN-1|cas 1262041-49-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: ASK1-IN-1|CAS: 1262041-49-5|Cat No: DC10781|Other Names: ASK IN 1

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.

ASK1-IN-1 dose-dependently decreases pulmonary arterial pressure and right ventricular (RV) hypertrophy in an in vivo model of pulmonary hypertension (PH). ASKl inhibition reduces hallmarks of pulmonary vascular disease including and not limited to reduce pulmonary vascular resistance (PVR), improve pulmonary pressure, decreased pulmonary vascular remodeling, improved vascular function, decrease maladaptive RV hypertrophy, and improve RV function. Inhibition of ASKl signaling may slow, prevent, and/or reverse pathological changes associated with PH. Plasma levels of B-type natriuretic peptide (BNP) are reduced by both doses of ASK1-IN-1: 0.1+0.05 for 0.1% and 0.1±0.1 ng/mL for 0.2%. Su/Hx rats treated with 0.1 % or 0.2% ASK1-IN-1 has a decreased number of completely muscularized arterioles (35.6% and 32.6%, respectively).


ALB-127158(a)|ALB-127158 A|cas 1173154-32-9

ALB-127158(a)|ALB-127158 A|cas 1173154-32-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: ALB-127158 A|CAS: 1173154-32-9|Cat No: DC10780|Other Names: ALB-127158A; ALB 127158A; ALB127158A; ALB-127158(a); ALB127158(a); ALB 127158(a); ALB-127158; ALB 127158; ALB127158,1173154-32-9

ALB-127158A, also known as ALB-127158(a), is a MCH1 antagonist for the treatment of obesity.

reclinical studies demonstrated that the compound produced significant weight loss in rodents. ALB-127158(a) may be a potential treatment for IBD. This example demonstrates how using data from the preclinical studies is possible to build decision points into an early clinical development plan that will allow early assessment of potential efficacy and allow timely go/no go decisions.The study, comprising the single ascending dose (SAD) and 14-day multiple ascending dose (MAD) arms, included standard safety assessments, ECG monitoring, and PK measurements. ALB-127158(a) was well tolerated in both the SAD and the MAD. Reported events were mild and showed little dose relationship.

PF-06651600|PF06651600|cas 1792180-81-4

PF-06651600|PF06651600|cas 1792180-81-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: PF-06651600|CAS: 1792180-81-4|Cat No: DC10779|Other Names: PF-06651600,PF 06651600,PF06651600

PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.

PF-06651600 is a potent and selective JAK3 inhibitor. PF-06651600), a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies


YKL-06-061|cas2172617-15-9 |SIK inhibitor

YKL-06-061|cas:2172617-15-9 |SIK inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: YKL-06-061|CAS: 2172617-15-9 |Cat No: DC10778|Other Names: YKL-06-061; YKL06-061; YKL 06-061; YKL-06061; YKL06061; YKL 06061

YKL-06-061 is a potent and selective SIK (salt-inducible kinase) inhibitor.

YKL-06-061 is a potent and selective SIK (salt-inducible kinase) inhibitor. Salt-inducible kinases (SIKs) are related to the metabolic regulator AMP-activated protein kinase (AMPK). Salt-inducible kinase induces cytoplasmic histone deacetylase 4 to promote vascular calcification. Pharmacologic inhibition of SIK sends HDAC4 to the nucleus and inhibits the calcification process in VSMCs, aortic rings, and in vivo In the cytoplasm, HDAC4 binds and its activity depends on the adaptor protein ENIGMA (Pdlim7) to promote vascular calcification.

Leonurine|cas 24697-74-3|Supplied by DC Chem

Leonurine|cas 24697-74-3|Supplied by DC Chem

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Product Name: Leonurine|CAS: 24697-74-3|Cat No: DC10777|Other Names:

Leonurine, a natural alkaloid extracted from Herba leonuri, has been proved to have anti-inflammatory effect.

Leonurine can obviously attenuate the spontaneous excitatory postsynaptic current amplitude and frequency on pyramidal neurons. Leonurine can dose-dependently suppress PI glycation. Leonurine may inhibit PI glycation through trapping MGO and keeping it from reacting with PI[2]. Leonurine can dose-dependently suppress PI glycation.Leonurine (60 mg/kg/day)+2-VO significantly decreases levels of glutamate and hydrogen peroxide, improves both the cognitive flexibility and the spatial learning and memory abilities. Moreover, leonurine obviously enhances long-term depression, elevates the ratio of N-methyl-D-aspartate receptor 2A/2B, and decreases the expression of postsynaptic density protein-95. Interestingly, the ratio of LC3II/LC3I and beclin-1 expression are markedly down-regulated by leonurine. Leonurine significantly alleviates LPS-induced histopathological changes, downregulates the levels of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), upregulates the level of anti-inflammatory cytokine interleukin-10 (IL-10), and inhibits the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in mouse mastitis model. Leonurine inhibits the expression of Toll-like receptor 4 (TLR4) and the activation of nuclear factor-kappaB (NF-κB) and the phosphorylation of p38, extracellular signal-regulated kinase (ERK), and Jun N-terminal kinase (JNK).

Cordycepin|cas 73-03-0|Supplied by DC Chem

Cordycepin|cas 73-03-0|Supplied by DC Chem

DC Chemicals, Website:www.dcchemicals.com

Product Name: Cordycepin|CAS: 73-03-0|Cat No: DC10776|Other Names:

Cordycepin is an adenosine analogue, which is readily phosphorylated to its mono-, di-, and triphosphate intracellularly. It has a very potent anti-cancer, anti-oxidant and anti-inflammatory activities.




CYC065|CYC 065|cas 1070790-89-4

CYC065|CYC 065|cas 1070790-89-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: CYC065|CAS: 1070790-89-4 |Cat No: DC10775|Other Names: CYC065; CYC-065; CYC 065,1070790-89-4

CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities.

CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow.

AZD5153|AZD5153|cas 1869912-39-9

AZD5153|AZD5153|cas 1869912-39-9 

DC Chemicals, Website:www.dcchemicals.com.

Product Name: AZD5153|CAS: 1869912-39-9 |Cat No: DC10774|Other Names: AZD5153; AZD-5153; AZD 5153

AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor.

AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor. AZD5153 exhibited excellent pharmacokinetic profile and exhibited high potency in vitro and in vivo effecting c-Myc downregulation and tumor growth inhibition in xenograft studies. AZD5153 showed enhanced potency as a result of bivalent binding and a clear correlation between BRD4 activity and cellular potency.


AZD5069|AZD-5069|cas 878385-84-3

AZD5069|AZD-5069|cas 878385-84-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: AZD5069|CAS: 878385-84-3|Cat No: DC10773|Other Names: AZD-5069; AZD 5069; AZD5069,878385-84-3

AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.

AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD. AZD-5069 was shown to inhibit binding of radiolabeled CXCL8 to human CXCR2 with a pIC50 value of 9.1. Furthermore, AZD5069 inhibited neutrophil chemotaxis, with a pA2 of approximately 9.6, and adhesion molecule expression, with a pA2 of 6.9, in response to CXCL1. AZD5069 was a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics. AZD-5069 is also potential useful for patient in inflammatory conditions.

Lanifibranor(IVA-337)|cas 927961-18-0

Lanifibranor(IVA-337)|cas 927961-18-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Lanifibranor|CAS: 927961-18-0 |Cat No: DC10772|Other Names: Lanifibranor; IVA-337; IVA 337; IVA337

Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.

Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσand PPARγ. Skin fibrosis is attenuated by Lanifibranor (IVA337) (p<0.05, vehicle vs Lanifibranor at 30 mg/kg and p<0.001, vehicle vs Lanifibranor at 100 mg/kg). Both low and high doses of Lanifibranor cause a significant decrease of collagenous matrix deposition. Administration of high (100 mg/kg) doses of Lanifibranor results in reduced body weight compare with vehicle controls (p<0.05; Lanifibranor at 100 mg/kg vs vehicle). Results demonstrate that activation of Peroxisome proliferator-activated receptors (PPARs) with Lanifibranor induces a significant reduction in the infiltration of macrophages, CD45+ leucocytes and lymphocytes in Lanifibranor-treated mice compare with rosiglitazone-treated counterparts.

CU-CPT-9m|cas 125079-83-6|TLR8 inhibitor

CU-CPT-9m|cas 125079-83-6|TLR8 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: CU-CPT-9m|CAS: 125079-83-6|Cat No: DC10771|Other Names: CU-CPT-9m,cas 125079-83-6 ,TLR8 inhibitor

CU-CPT-8m is a nolve TLR8 inhibitor.


CU-CPT-9b|cas 2165340-32-7|TLR8 inhibitor

CU-CPT-9b|cas 2165340-32-7|TLR8 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: CU-CPT-9b|CAS: 2165340-32-7 |Cat No: DC10770|Other Names: CU-CPT-9b,cas 2165340-32-7 ,TLR8 inhibitor

CU-CPT-9b is a nolve TLR8 inhibitor.


CU-CPT-9a|cas 2162962-69-6|TLR8 inhibitor

CU-CPT-9a|cas 2162962-69-6|TLR8 inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: CU-CPT-9a|CAS: 2162962-69-6|Cat No: DC10769|Other Names: CU-CPT-9a,cas 2162962-69-6,TLR8 inhibitor

CU-CPT-9a is a nolve TLR8 inhibitor.


IT 901|IT901|cas 1584121-99-2

IT 901|IT901|cas 1584121-99-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: IT 901|CAS: 1584121-99-2|Cat No: DC10768|Other Names: IT 901,IT901,IT-901,1584121-99-2

IT 901 is a c-Rel inhibitor (IC50 = 3 μM). Inhibits IL-2 expression in activated T-cells in vitro.


PQR530|PQR-530|cas 1927857-61-1

PQR530|PQR-530|cas 1927857-61-1 

DC Chemicals, Website:www.dcchemicals.com

Product Name: PQR530|CAS: 1927857-61-1 |Cat No: DC10767|Other Names: PQR530,PQR 530,PQR-530

PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor.

PQR530 is a novel, ATP site directed inhibitor of all PI3K isoforms and the mammalian target of rapamycin (mTOR) complexes C1/2 that is currently in pre-clinical development. PQR530 potently binds to its targets, inhibits cell proliferation and shows excellent selectivity versus related and unrelated kinases. PQR530 inhibits PI3K signaling in stimulated MCF7 cells as detected by PathScan analysis. Excellent tolerability has been found for PQR530 during GLP toxicological testing in rats and dogs. Increase in insulin and blood glucose, a treatable class effect of PI3K inhibitors, has been observed after PQR530 administration to mice. Investigation of mutagenicity and hERG binding resulted in a clean profile. PQR530 exhibited dose-proportional pharmacokinetics (PK) in male C57BL/6J mice. A maximum concentration (Cmax) in plasma and brain was reached after 30 minutes (7.8 μg/ml and 112.6 μg/ml, respectively) indicating that efficacious concentrations were reached in both tissues. The calculated half-life (t1/2) for plasma and brain was approximately 5 hours. PQR530 potently inhibited PI3K signaling in vivo for several hours after administration of a single oral dose of 50 mg/kg. Tumor growth was significantly decreased in SUDHL-6 lymphoma, RIVA lymphoma and OVCAR-3 ovarian cancer mouse xenografts using daily, oral administration. Conclusion: PQR530 is a potent, ATP competitive pan-PI3K and mTORC1/2 inhibitor. The physico-chemical properties of PQR530 result in good oral bioavailability and excellent brain penetration. PQR530 is well tolerated and efficiently inhibits tumor growth in xenograft models. Preclinical data allow for further development of the compound.

Verucerfont,GSK561679|GSK-561679

Verucerfont,GSK561679|GSK-561679

DC Chemicals, Website:www.dcchemicals.com

Product Name: Verucerfont,GSK561679|CAS: 885220-61-1|Cat No: DC10766|Other Names: Verucerfont,GSK561679,GSK-561679,GSK 561679,1610954-97-6

Verucerfont(GSK561679) is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316 311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)


LX2761|LX-2761|cas 1610954-97-6

LX2761|LX-2761|cas 1610954-97-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: LX-2761|CAS: 1610954-97-6 |Cat No: DC10765|Other Names:  LX2761; LX-2761; LX 2761,1610954-97-6

LX2761 is a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.

LX2761 is a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control. LX2761 has hSGLt1 2.2 nM; hSGLT2 2.7 nM and F% =<2. LX2761 is a very potent, chemically stable, and luminally restricted molecule that achieved proof of concept in OGTT at very low doses. LX2761 was designed to remain in the intestine after oral delivery to inhibit SGLT1 locally without affecting the SGLT1/2 mechanism in the kidney.

Theliatinib (HMPL-309)|EGFR inhibitor

Theliatinib (HMPL-309)|EGFR inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: Theliatinib (HMPL-309)|CAS: N/A|Cat No: DC10764|Other Names: HMPL-309,HMPL 309,HMPL309

Theliatinib (HMPL-309) is a novel small molecule, EGFR tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities.

Theliatinib (HMPL-309) is a novel small molecule, epidermal growth factor receptor tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities. Theliatinib is being developed as an oral formulation for the treatment of solid tumors like non-small cell lung cancer.Theliatinib pre-clinical studies were conducted in China. In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity and in vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. Non-clinical safety studies have indicated that Theliatinib is generally well tolerated in animals.

PhTx-74,Philanthotoxin 74|CAS 1227301-51-0

PhTx-74,Philanthotoxin 74|CAS 1227301-51-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Philanthotoxin 74 (hydrochloride)|CAS: 1227301-51-0|Cat No: DC10763|Other Names: PhTx 74 dihydrochloride

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

Philanthotoxin 74 (PhTx-74) is a synthetic analog of the naturally-occurring wasp venom toxin philanthotoxin-4,3,3. It is a subtype-selective AMPA receptor antagonist that inhibits homomeric GluR1 and GluR3 as well as heteromeric GluR1/2 receptors (80-100% of glutamate-evoked currents inhibited at 100 µM). It exhibits minimal to no effect on monomeric GluR2 or heteromeric GluR2/3 receptors at concentrations up to 500 µM. PhTx-74 inhibits the GluR5(Q) receptor with a Ki value of 0.29 µM.

Edonerpic maleate|T817|CAS#519187-23-6

Edonerpic maleate|T817|CAS#519187-23-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: Edonerpic maleate|CAS: 519187-23-6|Cat No: DC10762|Other Names: T-817; T 817; T817; CAS#519187-23-6, Edonerpic; Edonerpic maleate

Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).

Edonerpic, also known as T-817, is a neuroprotectant. Edonerpic is a candidate therapeutic agent for Alzheimer's disease that inhibits oxidative stress and nitric oxide-induced neurotoxicity and acts as a neurotrophic factor. Edonerpic protects against MPTP-induced neurotoxicity by blocking lipid peroxidation in the SNc, and imply that this compound may be useful for treating neurodegenerative disorders related to oxidative stress, such as Parkinson's disease.


Toceranib|cas 500-89-0

Toceranib|cas 500-89-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Thiambutosin|CAS: 500-89-0|Cat No: DC10761|Other Names:


Pocapavir|SCH 48973|V074|146949-21-5

Pocapavir|SCH 48973|V074|146949-21-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: Pocapavir|CAS: 146949-21-5|Cat No: DC10760|Other Names: Pocapavir,SCH-48973; SCH48973; SCH 48973; V074; V 073; V-073; Pocapavir

Pocapavir is an investigational enterovirus (EV) capsid inhibitor.

Pocapavir, also known as SCH-48973 and V-073, is a potent, selective, antienterovirus agent. SCH-48973 had antiviral activity (50% inhibitory concentrations [IC50s]) of 0.02 to 0.11 microg/ml, with no detectable cytotoxicity at 50 microg/ml. SCH-48973 inhibited 80% of 154 recent human enterovirus isolates at an IC50 of 0.9 microg/ml. The affinity constant (Ki) for SCH-48973 binding to poliovirus was 8.85 x 10(-8) M. SCH-48973 demonstrated efficacy in a murine poliovirus model of enterovirus disease. SCH-48973 represents a potential candidate for therapeutic intervention against enterovirus infections.


Roflumilast N-oxide|cas 292135-78-5

Roflumilast N-oxide|cas 292135-78-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: Roflumilast N-oxide|CAS: 292135-78-5|Cat No: DC10759|Other Names:

Roflumilast N-oxide is a phosphodiesterase 4 inhibitor. Roflumilast N-oxide is the active metabolite of roflumilast.

Roflumilast N-oxide is a phosphodiesterase 4 inhibitor. Roflumilast N-oxide is the active metabolite of roflumilast. Roflumilast N-Oxide in Combination with Formoterol Enhances the Antiinflammatory Effect of Dexamethasone in Airway Smooth Muscle Cells. Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells.

LM22B-10|cas 342777-54-2

LM22B-10|cas 342777-54-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: LM22B-10|CAS: 342777-54-2|Cat No: DC10758|Other Names:

LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.

LM22B-10 exhibits maximum neurotrophic survival activity levels that are higher than those maximally achieved with BDNF (53 ± 7.2% above BDNF at 0.7 nM) and NT-3 (91 ± 8.6% above NT-3 at 0.7 nM) with an EC50 value of 200-300 nM. LM22B-10 (1000 nM) induces neurites of significantly larger average lengths, up to ∼40 μM. LM22B-10 (250-2000 nM) binds to TrkB-Fc and TrkC-Fc in a dose-dependent manner. LM22B-10 inhibits binding of BDNF to TrkB-expressing cells and NT-3 to TrkC-expressing cells. LM22B-10 promotes cell survival and functions preferentially through TrkB and TrkC. LM22B-10, but not BDNF or NT-3, promotes neurite outgrowth in an inhibitory environment. LM22B-10 induces patterns of Trk and downstream signaling activation that are distinct from those of BDNF and NT-3. LM22B-10 also induces TrkB, TrkC, AKT and ERK activation in hippocampal neurons in culture.LM22B-10 (0.5 mg/kg) activates TrkB, TrkC, AKT and ERK in C57BL/6J mice. LM22B-10 (50 mg/kg, i,p,) shows increased phosphorylation at TrkBY817 and TrkCY820. LM22B-10 activates synaptic TrkB and TrkC and increases pre- and post-synaptic proteins and spine density in aged mice.

PCI 29732,PCI29732|cas 330786-25-9

PCI 29732,PCI29732|cas 330786-25-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: PCI-29732|CAS: 330786-25-9|Cat No: DC10757|Other Names: PCI 29732,PCI29732,PCI-29732

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay. IC50 value: 8.2 nM [1] Target: Btk kinase PCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology assay. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase, probably due to the difference at the “gatekeeper” residue. In human CD20+ B cells stimulated at the BCR, PCI-29732 blocked the transcriptional up-regulation of a panel of B-cell activation genes that occurs within 6 h of stimulation. Pulse exposure to the reversible inhibitor PCI-29732 did not result in BCR inhibition.


PF-06291826(Tafamidis)|cas 594839-88-0

PF-06291826(Tafamidis)|cas 594839-88-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: PF-06291826(Tafamidis)|CAS: 594839-88-0|Cat No: DC10756|Other Names: Tafamidis,cas 594839-88-0,PF-06291826,PF06291826

Tafamidis is a novel specific transthyretin (TTR) stabilizer or dissociation inhibitor.

Tafamidis is a novel specific transthyretin (TTR) stabilizer or dissociation inhibitor. TTR is a tetramer that is responsible in transporting the retinol-binding protein-vitamin A complex and minimally transporting thyroxine in the blood. In TTR-related disorders such as transthyretin familial amyloid polyneuropathy (TTR-FAP), tetramer dissociation is accelerated that results in unregulated amyloidogenesis and amyloid fibril formation. Eventually the failure of autonomic and peripheral nervous system is induced.

LSZ102|LSZ-102|Estrogen Receptor Degrader(SERD)

LSZ102|LSZ-102|Estrogen Receptor Degrader(SERD)

DC Chemicals, Website:www.dcchemicals.com

Product Name: LSZ102|CAS: N/A|Cat No: DC10755|Other Names: LSZ102,LSZ-102,LSZ 102

LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.


LX2343|LX-2343|CAS 333745-53-2

LX2343|LX-2343|CAS 333745-53-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: LX-2343|CAS: 333745-53-2|Cat No: DC10754|Other Names: LX2343,LX-2343,LX 2343

LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance.

LX2343 effectively ameliorated the cognitive deficits in APP/PS1 mice, targeting both Aβ production and clearance.LX2343 was able to ameliorate both OS and tauopathy at the same time; LX2343 substantially reduced ROS accumulation similar to an antioxidant and restored mitochondrial function through stabilizing the mitochondrial membrane potential, maintaining mitochondrial morphological integrity, and increasing ATP biosynthesis. In addition, LX2343 also suppressed hyperphosphorylation of tau by inhibition of GSK-3β. Thus, the dual effect of LX2343 has emphasized its potential for breaking the cycle of OS and tauopathy.LX2343 rescued neuronal cells from apoptosis by maintaining the integrity of mitochondrial function and morphology, alleviating OS and the JNK/p38 pathway and regulating anti- and pro-apoptotic proteins. In addition, LX2343 also potently inhibited tau hyperphosphorylation by functioning as a non-ATP competitive inhibitor of GSK-3β.

GLPG-1837(ABBV-974)|GLPG1837|cas 1654725-02-6

GLPG-1837(ABBV-974)|GLPG1837|cas 1654725-02-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: GLPG-1837(ABBV-974)|CAS: 1654725-02-6|Cat No: DC10753|Other Names: GLPG-1837; GLPG 1837; GLPG1837; ABBV-974; ABBV 974; ABBV974,1654725-02-6

GLPG-1837(ABBV-974) is a novel cystic fibrosis transmembrane conductance regulator CFTR potentiator.

GLPG-1837, also known as ABBV-974, is a novel cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. GLPG1837 was generally safe and well tolerated in healthy subjects up to the highest dose of 800 mg twice daily for 2 weeks. GLPG1837 shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor, the first marketed potentiator.


CNDAC|TAS-109|CAS 134665-72-8

CNDAC|TAS-109|CAS 134665-72-8

DC Chemicals, Website:www.dcchemicals.com

Product Name: CNDAC HCl|CAS: 134665-72-8|Cat No: DC10752|Other Names: DFP-10917 Hydrochloride; TAS-109 Hydrochloride,CNDAC,TAS109,TAS 109

CNDAC (DFP-10917; TAS-109) is an orally available deoxycytosine nucleoside analog with potential antineoplastic activity.


M2698|MSC-2363318A|cas 1379545-95-5

M2698|MSC-2363318A|cas 1379545-95-5

DC Chemicals, Website:www.dcchemicals.com


Product Name: M2698(MSC-2363318A)|CAS: 1379545-95-5|Cat No: DC10751|Other Names: M2698; M-2698; M 2698; MSC-2363318A; MSC 2363318A; MSC2363318A

M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier.

M2698, also known as MSC-2363318A, is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier. M2698 was highly potent in vitro (IC50 1 nM for p70S6K, Akt1 and Akt3 inhibition; IC50 17 nM for pGSK3β indirect inhibition) and in vivo (IC50 15 nM for pS6 indirect inhibition), and relatively selective (only 6/264 kinases had an IC50 within 10-fold of p70S6K).

Voruciclib |CAS 1000023-04-0|P1446A05

Voruciclib |CAS 1000023-04-0|P1446A05

DC Chemicals, Website:www.dcchemicals.com

Product Name: Voruciclib|CAS: 1000023-04-0|Cat No: DC10750|Other Names: P1446A05, P1446A-05, P1446A 05, Voruciclib

Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.


M-3814(nedisertib)|CAS 1637542-33-6

M-3814(nedisertib)|CAS 1637542-33-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: M-3814(nedisertib)|CAS: 1637542-33-6|Cat No: DC10749|Other Names: MSC2490484A; MSC-2490484A; MSC 2490484A; M3814; M-3814; M 3814; nedisertib

M-3814(nedisertib) is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities.

M-3814(nedisertib) is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, the DNA-PK inhibitor MSC2490484A binds to and inhibits the activity of DNA-PK. This inhibits the ability of tumor cells to repair damaged DNA, which may lead to a reduction in cellular proliferation of cancer cells expressing DNA-PK.


NSC31205|NSC-31205|CAS 6320-51-0

NSC31205|NSC-31205|CAS 6320-51-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: NSC31205|CAS: 6320-51-0|Cat No: DC10748|Other Names: NSC31205,NSC-31205,NSC 31205

NSC 31205 is a PIM2/1 inhibitor.


KDU691|KDU-691|cas 1513879-19-0

KDU691|KDU-691|cas 1513879-19-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: ML355|CAS: 1532593-30-8|Cat No: DC10747|Other Names: ML 355,ML-355,ML355

ML355 is a potent and selective inhibitors of 12-Lipoxygenase(12-LOX) with IC50 of 0.34 μM, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties.

ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2. In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.

KDU691|KDU-691|cas 1513879-19-0

KDU691|KDU-691|cas 1513879-19-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: KDU691|CAS: 1513879-19-0|Cat No: DC10746|Other Names: KDU691,KDU-691,KDU 691,1513879-19-0

KDU691 is a PI4K inhibitor.


Adelmidrol|CAS 1675-66-7

Adelmidrol|CAS 1675-66-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: Adelmidrol|CAS: 1675-66-7|Cat No: DC10745|Other Names:

Adelmidrol is an anti-inflammatory ethanolamide derivative of azelaic acid.


Cambinol|CAS 14513-15-6

Cambinol|CAS 14513-15-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: Cambinol|CAS: 14513-15-6|Cat No: DC10744|Other Names:

Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.

ML335|ML-335|TREK-1/2 Activator|CAS 825658-06-8

ML335|ML-335|TREK-1/2 Activator|CAS 825658-06-8

DC Chemicals, Website:www.dcchemicals.com

Product Name: ml335|CAS: 825658-06-8|Cat No: DC10743|Other Names: ML335; ML-335; ML 335; TREK-1/2 Activator

ML335 is a selective activator of both TREK-1 and TREK-2.

ML335 is a potent and selective TREK-1/2 Activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.


Fer-1|Ferrostatin-1|CAS 347174-05-4

Fer-1|Ferrostatin-1|CAS 347174-05-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: Ferrostatin-1 (Fer-1)|CAS: 347174-05-4|Cat No: DC10742|Other Names: Fer-1,Fer 1,Fer1,Ferrostatin-1,Ferrostatin 1,Ferrostatin1

Ferrostatin-1 is a selective inhibitor of erastin induced ferroptosis with EC50 value of 60 nM.


HAMNO|NSC111847|cas 138736-73-9

HAMNO|NSC111847|cas 138736-73-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: HAMNO (NSC111847)|CAS: 138736-73-9|Cat No: DC10741|Other Names: HAMNO; CID 6335338, MLS000737724, NSC111847, NSC-111847; NSC111847

HAMNO is a novel protein interaction inhibitor of replication protein A (RPA).

HAMNO, also known as NSC-111847, is a potent and selective inhibitor of replication protein A (RPA) interactions with proteins involved in the replication stress response.

ELN484228|ELN-484228|cas 312-63-0

ELN484228|ELN-484228|cas 312-63-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: ELN484228|CAS: 312-63-0|Cat No: DC10740|Other Names: ELN484228,ELN-484228,ELN 484228.

ELN484228 is a blocker of α-synuclein which is a key protein in Parkinson’s disease.

ELN484228 is a cell-permeable alpha-Synuclein Blocker.

AZD4635(HTL1071)|AZD 4635|A2AR inhibitor

AZD4635(HTL1071)|AZD 4635|A2AR inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: AZD4635|CAS: 1321514-06-0|Cat No: DC10739|Other Names: AZD-4635; AZD 4635; AZD4635; HTL-1071; HTL 1071; HTL1071

AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.


ARS-1323|ARS1323|KRAS Inhibitor

ARS-1323|ARS1323|KRAS Inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: ARS-1323|CAS: 1698024-73-5|Cat No: DC10738|Other Names: ARS1323,ARS 1323,ARS-1323


ARS-1323 is a novel inhibitor of mutant K-ras G12C.



Tropifexor (LJN452)|cas 1383816-29-2

Tropifexor (LJN452)|cas 1383816-29-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: Tropifexor (LJN452)|CAS: 1383816-29-2|Cat No: DC10737|Other Names: LJN 452,LJN-452,LJN452

Tropifexor (LJN452) is a highly potent non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

Tropifexor (compound 1) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM. Robust induction of both BSEP and SHP genes is observed in primary cells by Tropifexor in a concentration-dependent manner. BSEP induction above vehicle (DMSO) control is observed at concentrations as low as 1 nM, while strong induction of SHP (15-fold above vehicle) is observed at 10 nM and modest induction of SHP at 1 nM (3-fold).Tropifexor demonstrates highly potent induction of SHP and FGF15 in the ileum as doses as low as 0.1 mg/kg. In the liver, robust induction of SHP is observed at 0.01 mg/kg of Tropifexor with maximal levels of gene induction achieved at 0.3 mg/kg. Expression of CYP8B1 mRNA following 14 day treatment with Tropifexor is already apparent at the lowest dose (0.003 mg/kg), and CYP8B1 gene expression is fully repressed at doses above 0.03 mg/kg. Treatment of rats with Tropifexor exhibits a clear dose-dependent increase in plasma FGF15 protein, with maximal levels of FGF15 detected at 7 h postdose. Treatment with Tropifexor for 14 days produces a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, resulting in a decrease of triglyceride levels to approximately 79% below the vehicle control group.


CaCC(inh)-A01|TMEM16 Blocker I|cas 407587-33-1

CaCC(inh)-A01|TMEM16 Blocker I|cas 407587-33-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: CaCC(inh)-A01|CAS: 407587-33-1|Cat No: DC10736|Other Names: TMEM16 Blocker I

CaCC(inh)-A01 is a non-selective inhibitor of calcium-activated chloride channels (CaCCs) that blocks ATP-stimulated chloride conductance in human salivary gland, intestinal, and bronchial epithelium (mean IC50 = 10 µM).

CaCC(inh)-A01 (30 µM) induces full vasorelaxation of preconstricted mouse isolated mesenteric arteries in the presence or absence of chloride.CaCC(inh)-A01 also attenuates CaCC TMEM16-A-induced proliferation in cancer cell lines through targeted degradation of the protein and reduces BKCa channel activity in human red blood cells.

Alovudine|POLG inhibitor

Alovudine|POLG inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: Alovudine|CAS: 25526-93-6|Cat No: DC10735|Other Names: Alovudine, MIV-310; CL-184824; MIV310; CL184824; MIV 310; CL 184824

Alovudine is a DNA polymerase subunit gamma-1 (POLG) inhibitor, shows promise for treating AML.

Alovudine is a dideoxynucleoside thymidine analogue, which when phosphorylated shows POLG inhibitory activity. Investigators from Medivir and their collaborators aimed to study the effects of alovudine in acute myeloid leukemia (AML) cells both in vitro and in vivo. The results showed that when OCI-AML2 cells were separately treated with alovudine and AraC, there was a reduction in the biogenesis of mtDNA and oxidative phosphorylation was impaired, as were cell growth and viability in alovudine-treated cells compared to AraC-treated cells. When alovudine was administered to AML mice (n = 10) (dosed at 50 mg/kg b.i.d. p.o.) for 11 days, it was shown that tumor volume was reduced in these mice compared to control mice (n = 10), as was tumor weight, showing a clear antileukemic activity. These results confirm alovudine to be a potent POLG inhibitor that impairs oxidative phosphorylation in AML, decreasing its growth both in vitro an in vivo

NU2058|NU-2058|cas 161058-83-9

NU2058|NU-2058|cas 161058-83-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: NU2058|CAS: 161058-83-9|Cat No: DC10734|Other Names: NU 2058,NU-2058,NU2058

NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.


Sutezolid (PNU-100480)|CAS 168828-58-8

Sutezolid (PNU-100480)|CAS 168828-58-8

DC Chemicals, Website:www.dcchemicals.com

Product Name: Sutezolid (PNU-100480)|CAS: 168828-58-8|Cat No: DC10733|Other Names: PNU-100480; U-100480; PF-02341272

Sutezolid (PNU-100480) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis.


Anavex-73|CAS 195615-83-9

Anavex-73|CAS 195615-83-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: AVex-73|CAS: 195615-83-9|Cat No: DC10732|Other Names: AE-37; AVex-73; Anavex-2-73; Anavex-273; AE37; AVex73; Anavex273; AE 37; AVex 73; Anavex 2 73; Anavex 273

AVex-73 is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease


Arecaidine but-2-ynyl ester tosylate (CAS 119630-77-2)

Arecaidine but-2-ynyl ester tosylate (CAS 119630-77-2)

DC Chemicals, Website:www.dcchemicals.com

Product Name: Arecaidine but-2-ynyl ester tosylate|CAS: 119630-77-2|Cat No: DC10731|Other Names:

Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.


Inarigivir(ORI-9020,SB-9000)

Inarigivir(ORI-9020,SB-9000)

DC Chemicals, Website:www.dcchemicals.com

Product Name: Inarigivir(ORI-9020,SB-9000)|CAS: 475650-36-3|Cat No: DC10730|Other Names: Inarigivir; ORI-9020; ORI 9020; ORI9020; SB-40; SB-9000; SB9000, SB-9000

Inarigivir(SB-9000) is a novel dinucleotide, evaluated in transgenic mice expressing hepatitis B virus (HBV), significantly reduced liver HBV DNA。

Inarigivir, also known as ORI-9020 and SB-9000, is a novel dinucleotide, evaluated in transgenic mice expressing hepatitis B virus (HBV), significantly reduced liver HBV DNA (P </= 0.001). Levels of HBeAg and HBsAg in serum and of HBcAg in liver were not affected by treatment. A minimal effective dosage was determined to be between 1.6 and 0.5 mg/kg of body weight/day, which was similar to that observed for adefovir dipivoxil.


Inarigivir soproxil|SB9200|SB-9200|antiviral HCV variants

Inarigivir soproxil|SB9200|SB-9200|antiviral HCV variants

DC Chemicals, Website:www.dcchemicals.com

Product Name: SB9200(Inarigivir soproxil)|CAS: 942123-43-5|Cat No: DC10729|Other Names: SB9200,SB 9200,SB-9200

SB9200(Inarigivir soproxil) is a novel agonist of innate immunity, shows potent antiviral activity against resistant HCV variants.

SB 9200 is a novel, first-in-class oral modulator of innate immunity that is believed to act via the activation of the RIG-I and NOD2 pathways. SB 9200 has broad-spectrum antiviral activity against RNA viruses including hepatitis C virus (HCV), norovirus, respiratory syncytial virus, and influenza and has demonstrated activity against hepatitis B virus (HBV) in vitro and in vivo. In phase I clinical trials in chronically infected HCV patients, SB 9200 has been shown to reduce HCV RNA by up to 1.9 log. SB 9200 is active against diverse HCV genotypes and is also effective against HCV derived from patients who relapse following direct-acting antiviral treatment, including viruses containing known NS5A resistance-associated sequences. These data confirm the broad antiviral activity of SB 9200 and indicate that it may have clinical utility in HCV patients who have failed to respond to current antiviral regimens.


Pibrentasvir(ABT-530)

Pibrentasvir(ABT-530)

DC Chemicals, Website:www.dcchemicals.com

Product Name: Pibrentasvir(ABT-530)|CAS: 1353900-92-1|Cat No: DC10728|Other Names: Pibrentasvir,ABT530,ABT 530,ABT530

Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.


Elafibranor(GFT505)|GFT-505

Elafibranor(GFT505)|GFT-505

DC Chemicals, Website:www.dcchemicals.com

Product Name: Elafibranor(GFT505)|CAS: 824932-88-9|Cat No: DC10727|Other Names: Elafibranor,GF T505,GFT-505,GFT505

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ.GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study. Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. GFT505 treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys.


OPC-21268,OPC21268|cas 131631-89-5

OPC-21268,OPC21268|cas 131631-89-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: OPC 21268|CAS: 131631-89-5|Cat No: DC10726|Other Names: OPC 21268,OPC-21268,OPC21268

OPC-21268 is a vasopressin 1 receptor antagonist potentially for the treatment of heart failure and hypertension.

OPC 21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors. Arginine vasopressin (AVP) is a hormone that plays an important part in circulatory and water homoeostasis. There are three AVP receptor subtypes: V1a, V1b, and V2 that all belong to the large rhodopsin-like G-protein-coupled receptor family.

ARS-1620|ARS1620|KRAS-G12C inhibitor

ARS-1620|ARS1620|KRAS-G12C inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: ARS-1620|CAS: 1698055-85-4|Cat No: DC10725|Other Names: ARS-1620,ARS 1620,ARS1620

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.ARS-1620 selectively induces tumor regression in patient-derived tumor models. ARS-1620, an atropisomeric selective KRASG12C inhibitor with desirable PK. KRAS dependency is more profound in vivo compared to 2D-monolayer cell culture. ARS-1620 is a valuable pharmacological tool to interrogate KRAS biology in vivo. ARS-1620 achieves rapid and sustained in vivo target occupancy to induce tumor regression. We use ARS-1620 to dissect oncogenic KRAS dependency and demonstrate that monolayer culture formats significantly underestimate KRAS dependency in vivo. This study provides in vivo evidence that mutant KRAS can be selectively targeted and reveals ARS-1620 as representing a new generation of KRASG12C-specific inhibitors with promising therapeutic potential.


AZD2098|AZD-2098|cas 566203-88-1

AZD2098|AZD-2098|cas 566203-88-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: AZD2098|CAS: 566203-88-1|Cat No: DC10724|Other Names: AZD 2098,AZD-2098,AZD2098

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.


CGP-71683A|CGP71683A|cas 192322-50-2

CGP-71683A|CGP71683A|cas 192322-50-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: ABT-702|CAS: 1188890-28-9|Cat No: DC10723|Other Names: abt-702,abt702,abt 702

ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase).

ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase). Displays oral activity in animal models of pain and inflammation.


CGP-71683A|CGP71683A|cas 192322-50-2

CGP-71683A|CGP71683A|cas 192322-50-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: CGP-71683A|CAS: 192322-50-2|Cat No: DC10722|Other Names: CGP-71683A; CGP 71683A; CGP71683A; UNII-45B73P82A3

CGP 71683A is a potent and highly selective non-peptide antagonist of the NPY Y(5) receptor in the study of obesity.



Gefapixant(AF-219,MK-7264)|cas 1015787-98-0

Gefapixant(AF-219,MK-7264)|cas 1015787-98-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Gefapixant(AF-219,MK-7264)|CAS: 1015787-98-0|Cat No: DC10721|Other Names: Gefapixant,AF-219,MK-7264,AF 219,MK 7264,AF219,MK7264

Gefapixant(AF-219,MK-7264) is novel P2X3 receptor antagonist.


Tomatidine Hydrochloride|cas 6192-62-7

Tomatidine Hydrochloride|cas 6192-62-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: Tomatidine hydrochloride|CAS: 6192-62-7|Cat No: DC10720|Other Names:

Tomatidine hydrochloride is a steriodal alkaloid structurally sumilar to cyclopamine (sc-200929) but does not inhibit hedgehog pathway. It can be employed as a negative control for cyclopamine (sc-200929) and KAAD-cyclopamine.


RGX-104|RGX104|cas 610318-03-1

RGX-104|RGX104|cas 610318-03-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: RGX-104|CAS: 610318-03-1|Cat No: DC10719|Other Names: RGX-104,RGX 104,RGX104

RGX-104 is an orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities.

RGX-104 is an orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities.  Upon oral administration, LXRbeta agonist RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells. LXRbeta, a member of the oxysterol receptor family, which is in the nuclear receptor family of transcription factors, plays a key role in cholesterol transport, glucose metabolism and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor cell types. The expression of the ApoE protein becomes silenced in human cancers as they grow, become invasive, and metastasize; ApoE silencing is related to reduced survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers to evade the immune system and recruit blood vessels.Study RGX-104-001 is a Phase 1, first-in-human, dose escalation and expansion study of RGX-104, an oral small molecule targeting the liver X receptor (LXR). RGX-104 activates LXR, resulting in depletion of both myeloid-derived suppressor cells (MDSCs) as well as tumor blood vessels. MDSCs block the ability of T-cells and other cells of the immune system from attacking tumors.

During the dose escalation stage, multiple doses and schedules of orally administered RGX-104 will be evaluated in patients with advanced solid tumors and lymphoma (i.e., locally advanced and unresectable, or metastatic) who have had progressive disease (PD) on available standard systemic therapies or for which there are no standard systemic therapies of relevant impact. In the expansion stage of the study, additional patients with melanoma, non-small cell lung cancer, epithelial ovarian carcinoma, or breast cancer will be treated at the MTD (or maximum tested dose if no MTD is identified, or dose below the MTD if there is evidence suggesting a more favorable risk/benefit profile) to provide further characterization of RGX-104 safety, efficacy, PK, and pharmacodynamics, including biomarkers of immunologic activity and LXR target activation.RGX-104 depletes both myeloid-derived suppressor cells (MDSCs) as well as tumor blood vessels. MDSCs block T-cells and other cells of the immune system from attacking tumors, resulting in immune evasion. Treatment with RGX-104 reverses immune evasion, resulting in robust anti-tumor activity in established animal models of various cancer types, including drug-resistant tumors. In pre-clinical models, RGX-104 has demonstrated remarkable single-agent activity as well as synergy with approved therapies, such as immune check-point inhibitors. RGX-104 is currently being evaluated in a Phase 1 clinical study.


VU6005649|VU-6005649|cas 2137047-43-7

VU6005649|VU-6005649|cas 2137047-43-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: VU6005649|CAS: 2137047-43-7|Cat No: DC10717|Other Names: VU6005649; VU-6005649; VU 6005649

VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.

VU6005649 is a potent and CNS Penetrant mGlu7/8 Receptor PAM (mGlu7, IC50 = 649 nM; mGlu4, IC50 = 10 nM; mGlu8, IC50 = 2.6nM). VU6005649 demonstrates in vivo efficacy in a mouse contextual fear conditioning model.


2018年5月17日星期四

Antrodin A|camphorata anhydride A

Antrodin A|camphorata anhydride A

DC Chemicals, Website:www.dcchemicals.com

Product Name: Antrodin A|CAS: 656830-24-9|Cat No: DC10716|Other Names: Antrodin A,camphorata anhydride A




LYN-1604||LYN1604|CAS: 2088939-99-3

LYN-1604||LYN1604|CAS: 2088939-99-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: LYN-1604|CAS: 2088939-99-3|Cat No: DC10715|Other Names: LYN-1604,LYN 1604,LYN1604

LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM).

LYN-1604 is a ULK1 agonist. Three amino acid residues (LYS50, LEU53, and TYR89) are key to the activation site of LYN-1604 and ULK1 by site-directed mutagenesis and biochemical assays. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 is bound to wild-type ULK1 with a binding affinity in the nanomole range (KD = 291.4 nM), but the ULK1Y89A mutant protein causes a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1K50A and ULK1L53A mutants.LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. LYN-1604 can directly activate ULK1, the initiator of autophagy, thereby inducing cell death to inhibit the growth of TNBC in vitro and in vivo.


Esonarimod (KE-298) |CAS: 101973-77-7

Esonarimod (KE-298) |CAS: 101973-77-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: Esonarimod (KE-298)|CAS: 101973-77-7|Cat No: DC10714|Other Names: Esonarimod,KE-298,KE 298,KE298

Esonarimod (KE-298) is a new antirheumatic drug.


S-methyl-KE-298|CAS: 143584-75-2

S-methyl-KE-298|CAS: 143584-75-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: S-methyl-KE-298|CAS: 143584-75-2|Cat No: DC10713|Other Names:

S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.

S-methyl-KE-298 is a methyl conjugate of deacetyl-KE-298 is plasma. In vitro protein binding of KE-298 and its plasma metabolites, deacetyl-KE-298 (M-1) and S-methyl-KE-298 (M-2), is high in rat (>97%), dog (>89%) and human plasma (>99%), respectively. KE-298 blocks this IL-1β-induced pro-MMP-2 activation and MT1-MMP expression, but does not affect IL-1β-induced tissue inhibitor of metalloproteinase-2 (TIMP-2) secretion from rheumatoid synovial cells. KE-298 inhibits MMP-1 production from rheumatoid arthritis (RA) synovial cells by affecting a transcription factor, AP-1. KE-298 inhibits the basal levels of MT1-MMP expression of unstimulated rheumatoid synovial cells.

LY334370|LY-334370|CAS: 182563-08-2

LY334370|LY-334370|CAS: 182563-08-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: LY334370|CAS: 182563-08-2|Cat No: DC10712|Other Names: LY334370,LY-334370,LY 334370.

LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.

ML327|ML-327|CAS: 1883510-31-3

ML327|ML-327|CAS: 1883510-31-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: ML-327|CAS: 1883510-31-3|Cat No: DC10711|Other Names: ML327,ML-327,ML 327

ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).


2018年5月16日星期三

Skp2 Inhibitor C1(SKPin C1)|CAS: 432001-69-9

Skp2 Inhibitor C1(SKPin C1)|CAS: 432001-69-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: Skp2 Inhibitor C1(SKPin C1)|CAS: 432001-69-9|Cat No: DC10710|Other Names: Skp2 Inhibitor C1,SKPin C1

Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.


DL-AP5 Sodium salt|CAS: 1303993-72-7

DL-AP5 Sodium salt|CAS: 1303993-72-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: D-LAP5.Na|CAS: 1303993-72-7|Cat No: DC10709|Other Names:

DL-AP5 is a Broad spectrum EAA antagonist.


DL-AP5|CAS: 76326-31-3

DL-AP5|CAS: 76326-31-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: DL-AP5|CAS: 76326-31-3|Cat No: DC10708|Other Names:

DL-AP5 is a Broad spectrum EAA antagonist.


DL-AP4|CAS: 20263-07-4

DL-AP4|CAS: 20263-07-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: DL-AP4|CAS: 20263-07-4|Cat No: DC10707|Other Names:

DL-AP4 is a Broad spectrum EAA antagonist.

Ehp-inhibitor-2|CAS: 861249-77-6

Ehp-inhibitor-2|CAS: 861249-77-6

DC Chemicals, Website:www.dcchemicals.com

Product Name: Ehp-inhibitor-2|CAS: 861249-77-6|Cat No: DC10706|Other Names:

A novel Ehp inhibitor

Ehp-inhibitor-1|CAS: 861249-59-4

Ehp-inhibitor-1|CAS: 861249-59-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: Ehp-inhibitor-1|CAS: 861249-59-4|Cat No: DC10705|Other Names:

A novel Ehp inhibitor

Asimadoline (EMD-61753|CAS: 153205-46-0

Asimadoline (EMD-61753|CAS: 153205-46-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Asimadoline (EMD-61753|CAS: 153205-46-0|Cat No: DC10704|Other Names: EMD-61753,EMD61753,EMD 61753

Asimadoline (EMD-61753) is a drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist.


NSC 6038|CAS: 2447-87-2

NSC 6038|CAS: 2447-87-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: NSC 6038|CAS: 2447-87-2|Cat No: DC10703|Other Names:

NSC 6038 is a bioactive compound.


OR59402;NSC 48107|CAS: 79606-45-4

OR59402;NSC 48107|CAS: 79606-45-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: OR59402;NSC 48107|CAS: 79606-45-4|Cat No: DC10702|Other Names:

OR59402;NSC 48107 is a bioactive compound.


Benzamide (NSC 404988)|CAS: 7461-38-3

Benzamide (NSC 404988)|CAS: 7461-38-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: Benzamide (NSC 404988)|CAS: 7461-38-3|Cat No: DC10701|Other Names:

Benzamide (NSC 404988) is a bioactive compound.


Seladelpar|CAS: 851528-79-5

Seladelpar|CAS: 851528-79-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: Seladelpar|CAS: 851528-79-5|Cat No: DC10700|Other Names:

Seladelpar, also known as MBX-8025 and RWJ-800025, is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist. MBX-8025 may have potential use for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis.


Probucol Disuccinate|CAS: 216168-45-5

Probucol Disuccinate|CAS: 216168-45-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: Probucol Disuccinate|CAS: 216168-45-5|Cat No: DC10699|Other Names:


CGP4540(Amoscanate)|CAS: 100990-46-3

CGP4540(Amoscanate)|CAS: 100990-46-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: CGP4540(Amoscanate)|CAS: 100990-46-3|Cat No: DC10698|Other Names: CGP-4540,CGP 4540,CGP4540,nithiocyamine

Amoscanate(nithiocyamine) is an experimental anthelmintic agent of the arylisothiocyanate class which was found to be highly effective in animals against the four major species of schistosomes which infect humans,and is also highly active against hookworm infection.


NSC 80538 |CAS: 370-26-3

NSC 80538 |CAS: 370-26-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: NSC 80538 |CAS: 370-26-3|Cat No: DC10697|Other Names: NSC 80538,NSC-80538,NSC80538

NSC 80538 is a bioactive compound.

U 19963 |CAS: 404-52-4

U 19963 |CAS: 404-52-4

DC Chemicals, Website:www.dcchemicals.com

Product Name: U 19963 |CAS: 404-52-4|Cat No: DC10696|Other Names: U 19963,U-19963 ,U19963

U 19963 is a bioactive compound.


NSC 191412|CAS: 370-16-1

NSC 191412|CAS: 370-16-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: NSC 191412|CAS: 370-16-1|Cat No: DC10695|Other Names: NSC-191412,NSC191412

NSC 191412 is a bioactive compound.

Loflucarban|CAS: 790-69-2

Loflucarban|CAS: 790-69-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: Loflucarban|CAS: 790-69-2|Cat No: DC10694|Other Names:

Loflucarban is an antiinfective drug


O-Butyryl timolol|CAS: 106351-79-5

O-Butyryl timolol|CAS: 106351-79-5

DC Chemicals, Website:www.dcchemicals.com

Product Name: O-Butyryl timolol|CAS: 106351-79-5|Cat No: DC10693|Other Names: Butyryltimolol; Butyryl timolol; Butyryl-timolol

Butyryltimolol is a lipophilic ester prodrug of timolol, a beta adrenergic blocer with antihypertensive and hemodynamic properties.

R162|CAS: 64302-87-0

R162|CAS: 64302-87-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: R162|CAS: 64302-87-0|Cat No: DC10692|Other Names: R162,R-162,R 162

R162 is an inhibitor of GDH activity and represses glioma cell growth.


Pyronaridine|CAS: 74847-35-1

Pyronaridine|CAS: 74847-35-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: Pyronaridine|CAS: 74847-35-1|Cat No: DC10691|Other Names:

Pyronaridine, also known as Malaridine, is an antimalarial drug.


SPI-112Me|CAS: 1243685-62-2

SPI-112Me|CAS: 1243685-62-2

DC Chemicals, Website:www.dcchemicals.com

Product Name: SPI-112Me|CAS: 1243685-62-2|Cat No: DC10690|Other Names: SPI112Me,SPI 112me,SPI112me

SPI-112Me is a prodrug for SPI-112, which preferentially inhibits the
PTPase activity of Shp2 over Shp1 and PTP1B by a factor of 20 in cell-free
assays.


4P-PDOT|CAS: 134865-74-0

4P-PDOT|CAS: 134865-74-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: 4P-PDOT|CAS: 134865-74-0|Cat No: DC10689|Other Names: 4-P-PDOT; 4PPDOT; 4P-PDOT; AH-024; 4-phenyl-2- propionamidotetralin.

4P-PDOT, also known as 4-phenyl-2- propionamidotetralin, is a MT2-receptor-specific antagonist. MT2 melatonin receptor may be a novel target for analgesic drug development.


Sematilide hydrochloride|CAS: 101526-62-9

Sematilide hydrochloride|CAS: 101526-62-9


DC Chemicals, Website:www.dcchemicals.com

Product Name: Sematilide hydrochloride|CAS: 101526-62-9|Cat No: DC10687|Other Names: Sematilide hydrochloride; Sematilide HCl; Sematilide hydrochloride; Sematilide; CK-1752A; CK1752A; CK 1752A; CK-1752; CK1752; CK 1752.

Sematilide, also known as CK-1752, is a class III antiarrhythmic.


Cosan-528|CAS: 96686-51-0

Cosan-528|CAS: 96686-51-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Cosan-528|CAS: 96686-51-0|Cat No: DC10686|Other Names: Cosan-528; Cosan 528; Cosan528

Cosan-528 is a bioactive chemical.

Adipamidoxime(NSC 70868)|CAS: 15347-78-1

Adipamidoxime(NSC 70868)|CAS: 15347-78-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: Adipamidoxime(NSC 70868)|CAS: 15347-78-1|Cat No: DC10685|Other Names: NSC 70868,NSC-70868,NSC70868

Adipamidoxime(NSC 70868) is a new bioactive compoud.


QCC-374|CAS: 1356331-63-9

QCC-374|CAS: 1356331-63-9

DC Chemicals, Website:www.dcchemicals.com

Product Name: QCC-374|CAS: 1356331-63-9|Cat No: DC10684|Other Names: QCC-374; QCC 374; QCC374

QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.


DL 071-IT hydrochloride|CAS: 55104-39-7

DL 071-IT hydrochloride|CAS: 55104-39-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: DL 071-IT hydrochloride|CAS: 55104-39-7|Cat No: DC10683|Other Names: DL071-IT; DL-071-IT; DL 071-IT; DL 071-IT HCl; DL 071-IT hydrochloride.

DL 071-IT is a potent non-selective beta-adrenoceptor antagonist.


Velaresol|CAS: 77858-21-0

Velaresol|CAS: 77858-21-0

DC Chemicals, Website:www.dcchemicals.com

Product Name: Velaresol|CAS: 77858-21-0|Cat No: DC10682|Other Names: Velaresol; BW 12C79; BW-12C79; BW12C79; BW 12C; BW-12C; BW12C

Velaresol, also known as BW12C or BW12C79, is a oxyhaemoglobin stabilizer.


iCRT3|cas 901751-47-1|Wnt/β-catenin-responsive inhibitor

iCRT3|cas 901751-47-1|Wnt/β-catenin-responsive inhibitor

DC Chemicals, Website:www.dcchemicals.com

Product Name: iCRT3|CAS: 901751-47-1|Cat No: DC10680|Other Names: iCRT3,iCRT-3,iCRT 3

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.


EZM2302 (GSK3359088)|CARM1 inhibitor|EZM 2302

EZM2302 (GSK3359088)|CARM1 inhibitor|EZM 2302

DC Chemicals, Website:www.dcchemicals.com

Product Name: EZM2302 (GSK3359088)|CAS: N/A|Cat No: DC10679|Other Names: EZM2302,GSK3359088,EZM-2302,GSK-3359088,EZM 2302,GSK 3359088

EZM2302 (GSK3359088) is the first potent and selective inhibitor of CARM1 enzymatic activity that exhibits anti-proliferative effects both in vitro and in vivo,in biochemical assays (IC50=6nM) with broad selectivity against histone methyltransferases.

CARM1 is an arginine methyltransferase with diverse histone and non-histone substrates implicated in the regulation of cellular processes including transcriptional co-activation and RNA processing. CARM1 overexpression has been reported in multiple cancer types and has been shown to modulate oncogenic pathways in in vitro studies. Detailed understanding of the mechanism of action of CARM1 in oncogenesis has been limited by a lack of selective tool compounds, particularly for in vivo studies. Treatment of MM cell lines with EZM2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC50 values in the nanomolar range. Oral dosing of EZM2302 demonstrates dose-dependent in vivo CARM1 inhibition and anti-tumor activity in an MM xenograft model. EZM2302 (GSK3359088) is the first potent and selective inhibitor of CARM1 enzymatic activity that exhibits anti-proliferative effects both in vitro and in vivo,in biochemical assays (IC50=6nM) with broad selectivity against other histone methyltransferases. EZM2302 is a validated chemical probe suitable for further understanding the biological role CARM1 plays in cancer and other diseases.

Fluticasone|cas 90566-53-3|supplier DC Chemicals

Fluticasone|cas 90566-53-3|supplier DC Chemicals

DC Chemicals, Website:www.dcchemicals.com

Product Name: Fluticasone|CAS: 90566-53-3|Cat No: DC10678|Other Names:

Fluticasone is a synthetic glucocorticoid which is used in some countries to treat nasal symptoms.


SB-203580|SB203580|supplier DC Chemicals

SB-203580|SB203580|supplier DC Chemicals

DC Chemicals, Website:www.dcchemicals.com

Product Name: SB 203580 hydrochloride|CAS: 869185-85-3|Cat No: DC10677|Other Names: SB203580,SB 203580

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM and blocks PKB phosphorylation with IC50 of 3-5 μM.

For the detailed information about the solubility of SB-203580 in water, the solubility of SB-203580 in DMSO, the solubility of SB-203580 in PBS buffer, the animal experiment(test) of SB-203580,the in vivo,in vitro and clinical trial test of SB-203580,the cell experiment(test) of SB-203580,the IC50, EC50 and Affinity of SB-203580, please contact DC Chemicals.

Z-IETD-pNA(GRANZYME B SUBSTRATE I)|cas 498555-58-1

Z-IETD-pNA(GRANZYME B SUBSTRATE I)|cas 498555-58-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: Z-IETD-pNA(GRANZYME B SUBSTRATE I)|CAS: 498555-58-1|Cat No: DC10676|Other Names: Caspase-8 substrate (chromogenic), Granzyme B substrate (chromogenic), N-acetyl-Ile-Glu-Pro-Asp-pNA (p-nitroanilide)

Z-IETD-pNA is a colorimetric caspase-8/granzyme B substrate containing the benzyloxycarbonyl (Z) moiety.

Z-IETD-pNA is a colorimetric caspase-8/granzyme B substrate containing the benzyloxycarbonyl (Z) moiety. This substrate is hydrlyzed by caspase 8 to generate highly colored pNA that is measured at 405 nm by an absorption microplate reader or spectrophotometer.Fluorogenic substrate for caspase-8 and granzyme B with increased cell permeability. Also substrate for caspase-10.

LY3200882|LY-3200882|cas 1898283-02-7

LY3200882|LY-3200882|cas 1898283-02-7

DC Chemicals, Website:www.dcchemicals.com

Product Name: LY3200882|CAS: 1898283-02-7|Cat No: DC10675|Other Names:

LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.

LY3200882 is a next generation small molecule inhibitor of TGF-β receptor type 1 (TGFβRI). The molecule is a potent, highly selective inhibitor of TGFβRI embodied in a structural platform with a synthetically scalable route. It is an ATP competitive inhibitor of the serine-threonine kinase domain of TGFβRI. Mechanism of action studies reveal revealed that LY3200882 inhibits various pro-tumorigenic activities. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. In preclinical tumor models, LY3200882 showed potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment. Durable tumor regressions in the orthotopic 4T1-LP model were observed and rechallenge of congenic tumors resulted in complete rejection in all mice. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naïve T cell activity and restore proliferation. Therefore, LY3200882 shows promising activity as an immune modulatory agent. In addition, LY3200882 has shown anti-metastatic activity in vitro in migration assays as well as in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer). Finally, LY3200882 shows combinatorial anti-tumor benefits with checkpoint inhibition (anti-PD-L1) in the syngeneic CT26 model. In conclusion, we have developed a novel potent and highly selective small molecule inhibitor of TGFβRI for the treatment of cancer.

Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. Available from: https://www.researchgate.net/publication/318798009_Abstract_955_LY3200882_a_novel_highly_selective_TGFbRI_small_molecule_inhibitor [accessed Jan 02 2018].