Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-2-one
CDK inhibitor (pan-specific)
Molecular Weight:
241.25
Purity:
>98% by HPLC NMR (Conforms)
Form:
Orange solid
CAS Number:
[377090-84-1]
Formula:
C13H11N3O2
Application Notes:
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.
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