Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KenPaullone (9-Bromopaullone) 是一种CDK1/cyclin B 和GSK-3β抑制剂,IC50值分别为 0.4 μM 和 23 nM。它也抑制 CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p25 的活性,IC50值分别为 0.68 μM、7.5 μM 和 0.85 μM。。它通过增强 TGFβ-Smad3 信号通路增加和延长 foxp3 基因的转录来促进 iTreg 细胞分化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 262 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 867 | 现货 | ||
25 mg | ¥ 1,730 | 现货 | ||
50 mg | ¥ 2,810 | 现货 | ||
100 mg | ¥ 4,170 | 现货 | ||
500 mg | ¥ 9,070 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway. |
靶点活性 | CDK5-p35:0.85μM, CDK2-CyclinE:7.5μM, CDK2-CyclinA:0.68μM, CDK1-CyclinB:0.4μM, GSK-3β:0.23μM |
体外活性 | In HEK-293 cells, phosphorylation of the endogenous GSK3α on Tyr279 is greatly decreased after prolonged incubation with Kenpaullone. Also, the Phosphorylation of the endogenous GSK3β also decreases, although less markedly. Kenpaullone also induces the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. Kenpaullone (20 μM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli[2][3]. |
激酶实验 | IC50 determination: Active GST-LRRK2 (1326-2527), GST-LRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2527) and GST-LRRK2 [A2016T+G2019S] (1326-2527) enzyme is purified with glutathione sepharose from HEK293 cell lysate 36 h following transient transfection of the appropriate cDNA constructs. Peptide kinase assays, performed in duplicate, are set up in a total volume of 40 μL containing 0.5 μg LRRK2 kinase (which at approximately 10% purity gives a final concentration of 8 nM) in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 10 mM MgCl2, 20 μM Nictide, 0.1 μM [γ-32P]ATP (~500 cpm/pmol) and the indicated concentrations of inhibitor dissolved in DMSO. After incubation for 15 min at 30 °C, reactions are terminated by spotting 35 μL of the reaction mix onto P81 phosphocellulose paper and immersion in 50 mM phosphoric acid. Samples are washed extensively and the incorporation of [γ-32P]ATP into Nictide is quantified by Cerenkov counting. IC50 values are calculated with GraphPad Prism using non-linear regression analysis. |
别名 | 9-Bromopaullone, NSC-664704, 9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮 |
分子量 | 327.18 |
分子式 | C16H11BrN2O |
CAS No. | 142273-20-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 1.6 mg/mL (5 mM)), Heating is recommended.
DMSO: 32.7 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.0564 mL | 15.2821 mL | 30.5642 mL | 76.4105 mL |
5 mM | 0.6113 mL | 3.0564 mL | 6.1128 mL | 15.2821 mL | |
DMSO | 10 mM | 0.3056 mL | 1.5282 mL | 3.0564 mL | 7.6411 mL |
20 mM | 0.1528 mL | 0.7641 mL | 1.5282 mL | 3.8205 mL | |
50 mM | 0.0611 mL | 0.3056 mL | 0.6113 mL | 1.5282 mL | |
100 mM | 0.0306 mL | 0.1528 mL | 0.3056 mL | 0.7641 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KenPaullone 142273-20-9 Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells GSK-3 CDK Glycogen synthase kinase 3 NSC 664704 9-Bromopaullone inhibit NSC-664704 Inhibitor NSC664704 9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮 Cyclin dependent kinase Glycogen synthase kinase-3 inhibitor