Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC50=22nM), CDK1/cyclin B (IC50=40nM) and CDK4/cyclin D1 (IC50=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.
Product Details
| Alternative Name: | 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one |
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| Formula: | C13H11N3O2 |
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| MW: | 241.3 |
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| CAS: | 377090-84-1 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | Yellow to orange solid. |
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| Solubility: | Soluble in DMSO (10mg/ml). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | +4°C |
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| Handling: | Protect from light. Packaged under inert gas. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett.
13, 1939 (2003),
Abstract;
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC
310, 1026 (2003),
Abstract;
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem. Pharmacol.
64, 1091 (2002),
Abstract;
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res.
61, 6170 (2001),
Abstract;
