W6134 | RORγ inhibitor | Probechem Biochemicals

Chemical Structure : W6134

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W6134 (RORγ covalent inhibitor 29)

货号: PC-21716Not For Human Use, Lab Use Only.

W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.

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生物&药学活性

W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.
W6134 displays no activities against RORα, RXRγ, and ERRγ (IC50>20 uM).
W6134 significantly suppresses the colony formation in C4-2B and 22Rv1 cell lines, dramatically induces apoptosis of C4-2B and 22Rv1 cells.
W6134 effectively inhibits RORγ-dependent transcriptional activity and RORγ-related gene transcription in CRPC cell lines.
W6134 (5 or 10 mg/kg, i.p.) demonstrates in vivo antitumor activity in 22RV1 cell-derived xenograft.

物理化学性质&存储条件

分子量	482.98
分子式	C25H23ClN2O4S
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	N-(2'-Chloro-4'-(2-(4-(ethylsulfonyl)phenyl)acetamido)-[1,1'-biphenyl]-2-yl)acrylamide

参考文献

1. Wei Fang, et al. J Med Chem. 2024 Jan 16. doi: 10.1021/acs.jmedchem.3c02063.

W6134 (RORγ covalent inhibitor 29)

生物&药学活性

物理化学性质&存储条件

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W6134 (RORγ covalent inhibitor 29)

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