Name | KSI-3716 |
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Description | KSI-3716 is a c-Myc inhibitor. |
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Related Catalog | |
Target |
c-Myc[1] |
In Vitro | KSI-3716 blocks c-MYC/MAX from forming a complex with target gene promoters. KSI-3716 effectively blocks complex formation in a dose dependent manner (IC50=0.84 μM). c-MYC mediated transcriptional activity is inhibited by KSI-3716 at concentrations as low as 1 μM. The expression of c-MYC target genes, such as cyclin D2, CDK4 and hTERT, is markedly decreased. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis[1]. |
In Vivo | Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity[1]. |
Cell Assay | Ku19-19 cells are seeded 1 day before drug treatment and treated with KSI-3716 (5, 10, 15, 20, 25 μM) for (12, 24, 48 hours). Cell survival assays are performed to count viable cells[1]. |
Animal Admin | Mice[1] [1]The control group is administered solvent and the experimental group (5 tumor bearing mice per group) is administered c-MYC inhibitor KSI-3716 (5 mg/kg) intravesically twice weekly for 3 weeks. Luminescence images are obtained twice weekly[1]. |
References |
Molecular Formula | C17H11BrCl2N2O2 |
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Molecular Weight | 426.09 |