Apoptozole

Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with K_ds of 0.21 and 0.14?μM, respectively, and can induce apoptosis. IC50 & Target: Kd: 0.21 μM (Hsc70), 0.14?μM (Hsp70)^[1] In Vitro: Apoptozole is an inhibitor of Hsc70 and Hsp70, which binds to Hsc70 and Hsp70, with K_ds of 0.21 and 0.14?μM, respectively. Apoptozole (Apoptosis Activator VII; 1?μM) induces apoptosis in P19 cells. Apoptozole shows inhibitory activities against several cancer cell lines, such as SK-OV-3 (ovarian cancer cells), HCT-15 (colon cancer cells), and A549 (lung cancer cells), with IC₅₀s of 0.22, 0.25, and 0.13?μM, respectively^[1]. Apoptozole binds to the ATPase domain of Hsc70 and Hsp70, but does not binds to other types of heat shock proteins such as Hsp60, Hsp90 or Hsp40^[2]. Apoptozole (0-15 μM) suppresses the growth of A549 cells, HeLa cells, and MDA-MB-231 cells, with IC₅₀s ranging from 5 to 7 μM. Apoptozole (5 or 10 μM) shows no effect on associations of HSP70 with ASK1, JNK, or BAX, and does not induce AIF-mediated caspase-independent apoptosis in HeLa cells^[3]. In Vivo: Apoptozole (Apoptosis Activator VII; 4 mg/kg, i.p.) exhibits antitumor activities in nude mice xenografted with A549, RKO (colorectal carcinoma), and HeLa cells^[3].