SU-9516, CDK inhibitor (pan-specific) (TBI5705)

Description

Product Details

Formal Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one

Molecular Formula: C₁₃H₁₁N₃O₂

Formula Weight: 241.30

CAS Number: 377090-84-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

CDK inhibitor (pan-specific)

Functions

A cyclin-dependent kinase inhibitor, IC50s= 0.02-0.03, 0.04-0.2, 0.2-1.7 and 0.9 µM for cdk2, cdk1, cdk4, cdk9 respectively. Inhibits phosphorylation of retinoblastoma protein pRb, causing enhanced pRb/E2f complex formation, cell cycle arrest at G1 and G2-M and apoptosis. Down-regulates antiapoptotic protein Mcl-1 expression resulting in mitochondrial injury and cell death. Inhibits epithelial-mesenchymal transition (IC50=1.21 µM) a crucial pathological event in tumor cell budding and metastasis. Cell permeable.

Application Procedures

First dissolved in DMSO (25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.