KSI-3716

Names

[ CAS No. ]:
1151813-61-4

[ Name ]:
KSI-3716

Biological Activity

[Description]:

KSI-3716 is a c-Myc inhibitor.

[Related Catalog]:

Signaling Pathways >> Apoptosis >> c-Myc

Research Areas >> Cancer

[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]

[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.

[Related Small Molecules]

10058-F4 | KJ Pyr 9 | ML327 | 10074-G5 | Mycro 3

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₁BrCl₂N₂O₂

[ Molecular Weight ]:
426.09

Related Compounds

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