For research use only. Not for therapeutic Use.
SU9516（Cat No.:I003386）is a selective inhibitor of cyclin-dependent kinases (CDKs), particularly CDK2 and CDK4, which are crucial for cell cycle regulation. By inhibiting these kinases, SU9516 induces cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable compound in cancer research. It has shown efficacy in preclinical models against various tumor types, including breast and prostate cancers. Additionally, SU9516’s ability to target multiple CDKs positions it as a candidate for combination therapies, enhancing the effectiveness of existing treatments and providing insights into novel cancer therapeutic strategies.
| Catalog Number | I003386 |
| CAS Number | 377090-84-1 |
| Synonyms | 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one |
| Molecular Formula | C13H11N3O2 |
| Purity | ≥95% |
| Target | Cyclin-Dependent Kinases |
| Solubility | 10 mM in DMSO |
| Storage | Store at 4°C |
| IC50 | 22 nM/40 nM(CDK2/CDK1) [1] |
| IUPAC Name | (3Z)-3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one |
| InChI | InChI=1S/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)/b11-4- |
| InChIKey | QNUKRWAIZMBVCU-WCIBSUBMSA-N |
| SMILES | COC1=CC\2=C(C=C1)NC(=O)/C2=C\C3=CN=CN3 |
| Reference | </br>1:SU9516 Increases α7β1 Integrin and Ameliorates Disease Progression in the mdx Mouse Model of Duchenne Muscular Dystrophy. Sarathy A, Wuebbles RD, Fontelonga TM, Tarchione AR, Mathews Griner LA, Heredia DJ, Nunes AM, Duan S, Brewer PD, Van Ry T, Hennig GW, Gould TW, Dulcey AE, Wang A, Xu X, Chen CZ, Hu X, Zheng W, Southall N, Ferrer M, Marugan J, Burkin DJ.Mol Ther. 2017 Apr 5. pii: S1525-0016(17)30121-1. doi: 10.1016/j.ymthe.2017.03.022. [Epub ahead of print] PMID: 28391962 </br>2:CDK inhibitor SU9516 induces tetraploid blastocyst formation from parthenogenetically activated porcine embryos. Guo Q, Jin L, Zhu HY, Li XC, Zhang YC, Xing XX, Zhang GL, Xuan MF, Luo QR, Luo ZB, Wang JX, Kang JD, Yin XJ.Biotechnol Lett. 2017 Mar 17. doi: 10.1007/s10529-017-2321-6. [Epub ahead of print] PMID: 28315059 </br>3:A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516. Arai K, Eguchi T, Rahman MM, Sakamoto R, Masuda N, Nakatsura T, Calderwood SK, Kozaki K, Itoh M.PLoS One. 2016 Sep 13;11(9):e0162394. doi: 10.1371/journal.pone.0162394. eCollection 2016. PMID: 27622654 Free PMC Article</br>4:Cyclin-dependent kinase inhibitor SU9516 enhances sensitivity to methotrexate in human T-cell leukemia Jurkat cells. Uchiyama H, Sowa Y, Wakada M, Yogosawa M, Nakanishi R, Horinaka M, Shimazaki C, Taniwaki M, Sakai T.Cancer Sci. 2010 Mar;101(3):728-34. doi: 10.1111/j.1349-7006.2009.01449.x. Epub 2009 Nov 27. PMID: 20059476 Free Article</br>5: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. Gao N, Kramer L, Rahmani M, Dent P, Grant S.Mol Pharmacol. 2006 Aug;70(2):645-55. Epub 2006 May 3. PMID: 16672643 Free Article</br>6:SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2. Moshinsky DJ, Bellamacina CR, Boisvert DC, Huang P, Hui T, Jancarik J, Kim SH, Rice AG.Biochem Biophys Res Commun. 2003 Oct 24;310(3):1026-31. PMID: 14550307 </br>7:SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Yu B, Lane ME, Wadler S.Biochem Pharmacol. 2002 Oct 1;64(7):1091-100. PMID: 12234612 </br>8:A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Lane ME, Yu B, Rice A, Lipson KE, Liang C, Sun L, Tang C, McMahon G, Pestell RG, Wadler S.Cancer Res. 2001 Aug 15;61(16):6170-7. PMID: 11507069 Free Article |
