SU9516 | pan-specific CDK inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $258.00 |
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:
- Lane et al. (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells; Cancer Res. 61 6170
- Jorda et al. (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?; J. Med. Chem. 61 9105
- 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
- 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
- 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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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:
- Lane et al. (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells; Cancer Res. 61 6170
- Jorda et al. (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?; J. Med. Chem. 61 9105
- 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
- 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
- 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
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