Apoptozole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Apoptozole 是 Hsc70 和 Hsp70 ATPase 结构域的抑制剂，可诱导细胞凋亡。

Apoptozole, also known as Apoptosis Activator VII, is a selective inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity. Apoptozole enhances immune responses to administered antigens. Treatment of mice with Apoptozole elicits production of antibodies with a high IgG2c/IgG1 ratio and stimulates the release of Th1 and Th2-type cytokines, suggesting that Apoptozole activates the Th1 and Th2 immune responses. The ATPase activities of Hsp70 and Hsc70 are known to be responsible for regulation of various biological processes.

Apoptozole is an inhibitor of Hsc70 and Hsp70, which binds to Hsc70 and Hsp70, with Kds 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. 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. 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.

Apoptozole (Apoptosis Activator VII; 4 mg/kg, i.p.) exhibits antitumor activities in nude mice xenografted with A549, RKO (colorectal carcinoma), and HeLa cells.

Apoptozole | Apoptosis Activator VII

Others

Other Targets

HSC70| HSP70

Cancer

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1054543-47-3

625.56

C33H25F6N3O3

>98% (HPLC)

DMSO : ≥ 31 mg/mL; 49.56 mM

COC1=CC=C(C=C1)C2=C(N(C(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)CC4=CC=C(C=C4)C(=O)N)C5=CC=C(C=C5)OC

4-((2-(3,5-bis(trifluoromethyl)phenyl)-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl)methyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years