Hsp90-IN-15

Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP

Signaling Pathways >> Cell Cycle/DNA Damage >> HSP

HSP90

Hsp90-IN-15 (compound 22g) againsts HeLa, HepG2, and MDA-MB-23 cells with IC50s of 19.6 μM, 16.1 μM, and 22.1 μM, respectively[1]. Hsp90-IN-15 binds with Hsp90N, and the △Tm value is 10.92 °C[1]. Hsp90-IN-15 (0-20 μM; 48 h) arrests cell cycle at S phase in a dose-dependent manner[1]. Hsp90-IN-15 (0-20 μM; 48 h) exhibits an accumulation of early and late apoptotic cells in a time and dose dependent manner[1]. Caspase-3 is an executioner caspase and modifies apoptosis proteins[1]. Hsp90-IN-15 (0-50 μM; 48 h) increases the expression of Bax and cleaved-caspase 3, as well as downregulates the levels of Bcl-2, pro-caspase 3 and Hsp90[1]. Cell Viability Assay[1] Cell Line: HeLa cells Concentration: 0, 5, 10, 20 μM Incubation Time: 48 hours Result: Arrested cell cycle at S phase dose-dependently. Apoptosis Analysis[1] Cell Line: HeLa cells Concentration: 0, 5, 10, 20 μM Incubation Time: 48 hours Result: Induced apoptosis in HeLa cells. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0, 12.5, 25, 50 μM Incubation Time: 48 hours Result: Decreased the level of Hsp90 and increased the proportion of Bax/Bcl-2 as well.

[1]. Xu Y, et al. New modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment. Bioorg Med Chem. 2020 Feb 15. 28(4):115305.