VER-50589
| CAS No. | 747413-08-7 | Cat. No. | BCP09372 |
| Name | VER-50589 | ||
| Synonyms | VER50589;VER 50589; | ||
| Formula | C19H17ClN2O5 | M. Wt | 388.8 |
| Description | Hsp90 is an abundant protein with roles in protein folding, cell signaling, and cancer. VER-50589 is an isoxazole compound that inhibits Hsp90 with an IC50 value of 21 nM. It produces a mean cellular antiproliferative GI50 value of 78 nM when tested against a human cancer cell line panel. Consistent with inhibition of Hsp90, VER-50589 induces the expression of HSP27 and Hsp72 while reducing the client proteins C-RAF, B-RAF, survivin, and PRMT5, causing cell cycle arrest and apoptosis. VER-50589 shows favorable pharmacokinetics and impairs tumor growth in animals. Importantly, glioblastoma cells do not acquire resistance to VER-50589 and resistance to other Hsp90 inhibitors does not produce cross-resistance to VER-50589. | ||
| Pathways | Protease/Metabolic Enzyme Cell Cycle/DNA Damage | ||
| Targets | HSP | ||
Structure
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