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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-BAY-6092
BAY-6092

Chemical Structure : BAY-6092

CAS No.: 2413109-18-7

BAY-6092 (BAY6092)

货号: PC-22052Not For Human Use, Lab Use Only.

BAY-6092 (BAY6092) is a potent, selective YAP1/TAZ pathway inhibitor with IC50 of 1.6 nM in TEAD-luciferase assays, directly tareget PGGT1B, a subunit of the geranylgeranyltransferase-I (GGTase-I) complex.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BAY-6092 (BAY6092) is a potent, selective YAP1/TAZ pathway inhibitor with IC50 of 1.6 nM in TEAD-luciferase assays, directly tareget PGGT1B, a subunit of the geranylgeranyltransferase-I (GGTase-I) complex.
BAY-6092 potently inhibits human GGTase-I activity with biochemical IC50 of 64 nM.
BAY-6092 potently inhibits MDA-MB-231 and HT-1080 proliferation with IC50 of 49 and 9 nM respectively.
BAY-6092 effectively promoted YAP1 inactivation by translocation to the cytoplasm.
BAY-6092 dose-dependently down-regulates YAP1/TAZ target genes ANKRD1, CTGF, CYR61, CDC6, and DKK1.
BAY-6092 effectively inhibits GGTase-I substrates of the Rho-GTPase family in MDA-MB-231 cells, and causes YAP1/TAZ inactivation.
BAY-6092 impairs cancer cell proliferation and invasion in vitro with IC50 of <1 uM against a panel of cell lines from different tumor types.

物理化学性质&存储条件

分子量 490.52
分子式 C26H29F3N2O4
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

(R)-5-(2-methoxyphenyl)-9-((R)-3,3,3-trifluoro-2-methoxy-2-phenylpropanoyl)-3,9-diazaspiro[5.5]undecan-2-one

参考文献

1. Graham K, et al. Cell Chem Biol. 2024 Mar 19:S2451-9456(24)00087-4.

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