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Chemical Structure : W6134
Catalog No.: 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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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.
| M.Wt | 482.98 | |
| Formula | C25H23ClN2O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Wei Fang, et al. J Med Chem. 2024 Jan 16. doi: 10.1021/acs.jmedchem.3c02063.
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