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BAY-593

Chemical Structure : BAY-593

CAS No.: 2413020-56-9

BAY-593 (BAY593)

Catalog No.: PC-22050Not For Human Use, Lab Use Only.

BAY-593 (BAY593) is a potent, selective, in vivo-active YAP1/TAZ pathway inhibitor with IC50 of 9.4 nM in TEAD-luciferase assays, directly tareget PGGT1B, a subunit of the geranylgeranyltransferase-I (GGTase-I) complex.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BAY-593 (BAY593) is a potent, selective, in vivo-active YAP1/TAZ pathway inhibitor with IC50 of 9.4 nM in TEAD-luciferase assays, directly tareget PGGT1B, a subunit of the geranylgeranyltransferase-I (GGTase-I) complex.
BAY-593 potently inhibits MDA-MB-231 and HT-1080 proliferation with IC50 of 564 and 38 nM respectively.
BAY-593 effectively promoted YAP1 inactivation by translocation to the cytoplasm with an IC50 of 44 nM.
BAY-593 dose-dependently down-regulates YAP1/TAZ target genes ANKRD1, CTGF, CYR61, CDC6, and DKK1.
BAY-593 effectively inhibits GGTase-I substrates of the Rho-GTPase family in MDA-MB-231 cells, and causes YAP1/TAZ inactivation.
BAY-593 impairs cancer cell proliferation and invasion in vitro with IC50 of <1 uM against a panel of cell lines from different tumor types.
BAY-593 (5 mg/kg, BID or QD; 10 mg/kg QD, p.o.) reduces tumor growth in MDA-MB-231 human breast cancer tumors in female NMRI nu/nu mice.

Physicochemical Properties

M.Wt 476.54
Formula C26H31F3N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-3,3,3-trifluoro-2-methoxy-1-((R)-7-(2-methoxyphenyl)-3,9-diazaspiro[5.5]undecan-3-yl)-2-phenylpropan-1-one

References

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

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