2018年5月16日星期三

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].