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IC86621(DNA-PK Inhibitor III)404009-40-1

更新时间:2024-07-19

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简要描述:
IC86621(DNA-PK Inhibitor III)404009-40-1
上海一基实业有限公司是主要从事标准品、配套试剂的生产和销售的企业,产品用途:科研实验,标准对照品研究中心代理的作为一种衡量标准。

IC86621(DNA-PK Inhibitor III)404009-40-1

IC86621(DNA-PK Inhibitor III)
分子式:C12H15NO3   分子量:221.26
 
产品描述
IC86621(DNA-PK Inhibitor III)是一种新型DNA依赖的蛋白激酶催化亚基(DNA-PKcs)抑制剂,IC50为100 nM
靶点
PI 3-Kinase catalytic subunit p110b
DNA-PK-mediated cellular DNA DSB (double strand break) repair
      
IC50
135 nM
68 µM(EC50)
      
生物活性
A cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4, 0.88, and 1.0 µM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM
溶解性
DMSO ≥10 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO

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