Kenpaullone-9-Bromopaullone-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKenpaulloneCat. No.: HY-12302CAS No.: 142273-20-9Synonyms: 9-Bromopaullone; NSC-664704分式: CHBrNO分量: 327.18作靶点: CDK; GSK-3作通路: Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、 months-20C 1 month溶解性数据体外实验 DMSO : 35 mg/mL (106.97 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0564 mL 15.2821 mL 30.5642 mL5 mM 0.6113 mL 3.0564 mL 6.1128 mL10 mM 0.3056 mL 1.5282 mL 3.0564 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您

3、的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.64 mM); Suspended solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Ke

4、npaullone种有效的 CDK1/cyclin B 和 GSK-3 抑制剂，IC50 值分别为 0.4 M 和 23 nM，同时可抑制CDK2/cyclin A，CDK2/cyclin E 和 CDK5/p25 的活性，IC50 值分别为 0.68 M，7.5 M 和 0.85 M。IC50 & Target Cdk1/cyclin B cdk2/cyclin A CDK5/p35 CDK2/cyclinE0.4 M (IC50) 0.68 M (IC50) 0.85 M (IC50) 7.5 M (IC50)GSK-3 erk1 erk2 c-raf0.023 M (IC50) 20 M

5、 (IC50) 9 M (IC50) 38 M (IC50)体外研究 Kenpaullone shows much less effect on c-src (IC50, 15 M), casein kinase 2 (IC50, 20 M), erk 1 (IC50, 20 M), and erk 2 (IC50, 9 M). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent Ki is2.5 M. Kenpaullone can inhibit the growth of tumor ce

6、lls in culture (mean GI50, 43 M) and causes alteredcell cycle progression most clearly revealed under conditions of recovery from serum starvation 1.Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic cellsurvival and proliferation to the induction o

7、f apoptosis in cancer cells 2.PROTOCOLKinase Assay 1 The kinase assay is run for 10 min at 30C with 1 mg/mL histone H1, in the presence of 15 M g-32PATP(3000 Ci/mol; 1 mCi/mL) in a final volume of 30 ml. Purification and assays or inhibition of other kinases areperformed. In kinetic experiments, the

8、 histone H1 concentration is lowered to 3.5 mg/mL; the ATPconcentration ranged from 50 to 400 M, and the kenpaullone concentration ranges from 1 to 4 M.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zaharevitz DW, et al. Discovery and init

9、ial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9.2. Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. ProcNatl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.McePdfHeightCaution: Product has not been fully validated for med