GNF-2

一种Bcr-Abl的别构抑制剂（IC50 = 267 nM）；在10 µM浓度下对Bcr-Abl具有选择性抑制作用，相较于c-Abl及63种其他激酶；抑制Ba/F3细胞的增殖（IC50 = 138 nM）；在10 µM浓度下减少IBV感染的Vero细胞中的病毒滴度；在10和20 µM浓度下抑制LPS诱导的BV-2小胶质细胞中NO和TNF-α的生成；在小鼠炎症性疼痛模型中，1和20 mg/kg剂量下减少足肿胀并增加足撤回潜伏期；在STZ诱导的糖尿病神经病理模型中，减少机械性和热性痛觉过敏。An allosteric inhibitor of Bcr-Abl (IC50 = 267 nM); selective for Bcr-Abl over c-Abl and a panel of 63 additional kinases at 10 µM; inhibits proliferation of Ba/F3 cells (IC50 = 138 nM); reduces viral titers in IBV-infected Vero cells at 10 µM; inhibits LPS-induced production of NO and TNF-α in BV-2 microglia at 10 and 20 µM; reduces paw edema and increases the latency to paw withdrawal in a mouse model of inflammatory pain at 1 and 20 mg/kg; decreases mechanical and thermal hyperalgesia in a mouse model of STZ-induced diabetic neuropathy.