A potent inhibitor of several CDKs with selectivity for Cdk2 (IC50s = 22

SU 9516 – 1 mg

Brand:
Cayman
CAS:
377090-84-1
Storage:
-20
UN-No:
Non-Hazardous - /

SU 9516 is a 3-substituted indolinone that has anti-proliferative and pro-apoptotic activity in tumor cells. It is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1).{23507} It does not inhibit PKC, p38, PDGFR, or EGFR (IC50s = >10 µM).{23507} SU 9516 inhibits phosphorylation of the retinoblastoma protein pRb, resulting in increased pRb/E2F complex formation, cell-cycle arrest, and subsequent apoptosis.{23507,23508} In leukemia cells (U937, Jurkat, and HL-60 cells) SU 9516 downregulates transcription of the antiapoptotic protein Mcl-1, leading to mitochondrial injury and cell death.{23509}  

 

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Description

A potent inhibitor of several CDKs with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells

Formal name: 1,3-dihydro-3Z-(1H-imidazol-5-ylmethylene)-5-methoxy-2H-indol-2-one

Synonyms: 

Molecular weight: 241.3

CAS: 377090-84-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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