KSI-3716 is a c-Myc inhibitor used as a bladder chemotherapy agent. It blocks the formation of the c-MYC/MAX complex with the target gene promoter and induces cell cycle arrest and apoptosis. It can be used for bladder cancer research.

c-Myc:0.86 μM

KSI-3716 is a potent c-Myc inhibitor that blocks the binding of c-MYC/MAX to target gene promoters. KSI-3716 is used as an intravesical chemotherapy agent. KSI-3716 effectively blocks complex formation in a dose-dependent manner, IC50 0.86 μM. C-myc-mediated transcription activity was inhibited by KSI-3716 at concentrations as low as 1 μM. KSI-3716 has cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis. [1]

KSI-3716 was injected into the bladder of mice xenografted with bladder cancer at a dose of 5 mg/kg, and it was observed that it could significantly inhibit tumor growth and had little systemic toxicity. [1]