|
|
| | SU 9516 Basic information |
| | SU 9516 Chemical Properties |
| storage temp. | Store at +4°C | | solubility | DMSO: ~17 mg/mL | | form | crystalline | | color | brown |
| | SU 9516 Usage And Synthesis |
| Uses | SU 9516 is a 3-substituted indolinone CDK inhibitor with potent and selective inhibition towards cyclin-dependant kinases. | | Definition | ChEBI: 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one is a member of indoles. | | Biological Activity | Potent, selective cdk2 inhibitor (IC 50 values are 0.022, 0.04, >10, >10, 18 and >100 μ M for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G 1 and G 2 -M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro . | | references | [1]. lane me, yu b, rice a, et al. a novel cdk2-selective inhibitor, su9516, induces apoptosis in colon carcinoma cells. cancer res, 2001, 61(16): 6170-6177.
[2]. yu b, lane me, wadler s. su9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight e2f complexes in human colon carcinoma cells. biochem pharmacol, 2002, 64(7): 1091-1100.
[3]. gao n, kramer l, rahmani m, et al. 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, 2006, 70(2): 645-655. |
| | SU 9516 Preparation Products And Raw materials |
|