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

IC86621(DNA-PK Inhibitor III)
分子式：C12H15NO3   分子量：221.26
 
產(chǎn)品描述
IC86621(DNA-PK Inhibitor III)是一種新型DNA依賴的蛋白激酶催化亞基(DNA-PKcs)抑制劑，IC50為100 nM
靶點(diǎn)
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
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO