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Chemical Structure : BAY-856
Catalog No.: 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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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.
| M.Wt | 444.62 | |
| Formula | C29H36N2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Graham K, et al. Cell Chem Biol. 2024 Mar 19:S2451-9456(24)00087-4.
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