VER-50589

VER-50589是一种抑制Hsp90的异恶唑化合物，Hsp90是一种热休克蛋白，在分子折叠，细胞信号转导和癌症中起着分子伴侣的作用。| VER-50589是一种异恶唑化合物，已显示通过抑制Hsp90抑制Hsp90。 IC50值为21 nM。当针对人类癌细胞系进行测试时，它产生的平均细胞抗增殖GI50值为78 nM。与抑制Hsp90一致，VER-50589还显示出诱导HSP27和Hsp72的表达，同时减少了客体蛋白C-RAF，B-RAF，survivin和PRMT5，从而导致细胞周期停滞和凋亡。VER-5

VER-50589 is an isoxazole compound that inhibits Hsp90, a heat shock protein that acts as a molecular chaperone with roles in protein folding, cell signaling, and cancer.|VER-50589 is an isoxazole compound that has been shown to inhibit 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 has also been shown to induce 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.