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Submit ReviewSU 9516
说明： Cdk inhibitor; potently inhibits cdk1 and cdk2
化学名： (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one
纯度： ≥99% (HPLC)
生物活性 for SU 9516
SU 9516 is a cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.02 - 0.03, 0.04 - 0.2, 0.2 - 1.7 and 0.9 μM for cdk2, cdk1, cdk4 and cdk9, respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.
技术数据 for SU 9516
| 分子量 | 241.25 |
| 公式 | C13H11N3O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 377090-84-1 |
| PubChem ID | 5289419 |
| InChI Key | QNUKRWAIZMBVCU-WCIBSUBMSA-N |
| Smiles | O=C2NC1=CC=C(OC)C=C1/C2=C/C3=CNC=N3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for SU 9516
参考文献 for SU 9516
参考文献是支持产品生物活性的出版物。
Lane et al (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 61 6170 PMID: 11507069
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 PMID: 12234612
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 m Mol.Pharmacol. 70 645 PMID: 16672643
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem 61 9105 PMID: 30234987
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关键词: SU 9516, SU 9516 supplier, Potent, cdk2, inhibitors, inhibits, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Cyclin-dependent, Kinase, Non-selective, CDKs, 2907, Tocris Bioscience
2 篇 SU 9516 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SU 9516 的部分引用包括：
Pollet et al (2018) The AHR represses nucleotide excision repair and apoptosis and contributes to UV-induced skin carcinogenesis. Cell Death Differ 25 1823 PMID: 30013037
Shi et al (2014) The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis. J Cell Mol Med 18 2061 PMID: 25124967
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