KSI-3716是c-Myc的抑制剂。
货号:ajcx13038
CAS:1151813-61-4
分子式:C17H11BrCl2N2O2
分子量：426.09
溶解度:DMSO: 5 mg/mL (11.73 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KSI-3716 is a c-Myc inhibitor.

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].

Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity[1].

[1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.

Protocol:

Cell experiment:	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 experiment:	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].
参考文献: [1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.