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SU9516 | pan-specific CDK inhibitor

CAS:
SU9516
Catalog Number:
10-5705
Activity:
pan-specific CDK inhibitor
Chemical Names:
(Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-2-one
Molecular Weight:
241.25
Molecular Formula:
C13H11N3O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Orange solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

SU9516 (377090-84-1) is 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.1,2 Inhibits phosphorylation of retinoblastoma protein pRb, causing enhanced pRb/E2f complex formation, cell cycle arrest at G1 and G2-M and apoptosis.3 Down-regulates antiapoptotic protein Mcl-1 expression resulting in mitochondrial injury and cell death.4 Inhibits epithelial-mesenchymal transition (IC50=1.21 µM) a crucial pathological event in tumor cell budding and metastasis.5 Cell permeable.

References/Citations:

  1. Lane et al. (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells; Cancer Res. 61 6170
  2. Jorda et al. (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?; J. Med. Chem. 61 9105
  3. Yu et al. (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells; Biochem. Pharmacol. 64 1091
  4. Gao et al. (2006) The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism; Mol.  Pharmacol 70 645
  5. Arai et al. (2016) A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516; PLoS One 11 e0162394

 

 

SU9516 | pan-specific CDK inhibitor is also available in the Cellular Metabolism Library.
CAS:
SU9516
Catalog Number:
10-5705
Activity:
pan-specific CDK inhibitor
Chemical Names:
(Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-2-one
Molecular Weight:
241.25
Molecular Formula:
C13H11N3O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Orange solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

N/A
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