9-ING-41 是基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β 抑制剂,IC50为 0.71 μM。它显著导致癌细胞的细胞周期停滞,自噬和凋亡,具有增强化疗药物抗肿瘤作用的潜力,有抗癌活性。
产品描述
9-ING-41 is a glycogen synthase kinase-3 inhibitor.
体外活性
9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis[2]. 9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2]. 9-ING-41 (0.1-1 μM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker[1]. 9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM[2].
体内活性
In a mouse model of MCL, 9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity [2].
Cas No.
1034895-42-5
分子式
C22H13FN2O5
分子量
404.35
储存和溶解度
DMSO:97 mg/mL (239.89mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years