TMPRSS6 inhibitor Cpd-B

Chemical Structure : TMPRSS6 inhibitor Cpd-B

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货号: PC-73086Not For Human Use, Lab Use Only.

TMPRSS6 inhibitor Cpd-B (TMPRSS6-IN-Cpd-B) is a highly potent (IC50=7.6 nM), specific small molecule inhibitor of TMPRSS6 (matriptase-2).

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

TMPRSS6 inhibitor Cpd-B (TMPRSS6-IN-Cpd-B) is a highly potent (IC50=7.6 nM), specific small molecule inhibitor of TMPRSS6 (matriptase-2).
TMPRSS6 inhibitor Cpd-B shows no activity toward furin, wekaly inhibits other TTSP family members matriptase and hepsin, as well as factor Xa and thrombin.
TMPRSS6 inhibitor Cpd-B demonstrates cellualr IC50 (144 nM) in cell media of TMPRSS6-transfected HEK293 cells with no cytotoxicity, and no negatively affect TMPRSS6 plasma membrane localization.
Inhibiting TMPRSS6 proteolytic activity prevents cleavage of hemojuvelin (HJV) in HeLa cells (IC50=267 nM).
TMPRSS6 inhibition increases hepcidin encoding gene (HAMP) expression in HepG2 cells and human primary hepatocytes.
TMPRSS6, also known as matriptase-2, is a TTSP almost exclusively expressed at the surface of hepatocytes in the liver, and plays a key role in iron homeostasis via modulation of hepcidin expression.

物理化学性质&存储条件

分子量	636.265
分子式	C28H25BBrF2N7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(4-(6-((3-(aminomethyl)benzyl)amino)-9-(3-((4-bromophenyl)amino)-3-oxopropyl)-9H-purin-8-yl)-3,5-difluorophenyl)boronic acid

参考文献

1. Béliveau F, et al. Cell Chem Biol. 2019 Nov 21;26(11):1559-1572.e9.