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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-BAY-856
BAY-856

Chemical Structure : BAY-856

CAS No.: 2412709-24-9

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BAY-856 (BAY856)

货号: PC-22051Not For Human Use, Lab Use Only.

BAY-856 (BAY856) is a potent, selective YAP1/TAZ pathway inhibitor with IC50 of 49 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-856 (BAY856) is a potent, selective YAP1/TAZ pathway inhibitor with IC50 of 49 nM in TEAD-luciferase assays, directly tareget PGGT1B, a subunit of the geranylgeranyltransferase-I (GGTase-I) complex.
BAY-856 potently inhibits human GGTase-I activity with biochemical IC50 of 64 nM.
BAY-856 effectively promoted YAP1 inactivation by translocation to the cytoplasm with an IC50 of 44 nM.
BAY-856 dose-dependently down-regulates YAP1/TAZ target genes ANKRD1, CTGF, CYR61, CDC6, and DKK1 with IC50 of 0.09, 0.11, 0.13, 0.14, and 0.17 μM, respectively, in MDA-MB-231 cells, with no inhibition of control gene ACTB.
BAY-856 (1 uM) effectively inhibits GGTase-I substrates of the Rho-GTPase family in MDA-MB-231 cells, and causes YAP1/TAZ inactivation.
BAY-856 impairs cancer cell proliferation and invasion in vitro with IC50 of <1 uM against a panel of cell lines from different tumor types.
BAY-856 (125 mg/kg, BID; p.o.) reduced tumor growth in MDA-MB-231 human breast cancer tumors in female NMRI nu/nu mice.

物理化学性质&存储条件

分子量 444.62
分子式 C29H36N2O2
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)-9-(1-(3,5-dimethylphenyl)cyclopentane-1-carbonyl)-5-phenyl-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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