GW806742X 是ATP模拟物,是MLKL抑制剂,可结合 MLKL 假激酶结构域,Kd值为 9.3μM。它对VEGFR2的IC50为 2 nM,延缓 MLKL 膜移位并抑制坏死。
半岛bd体育手机客户端 描述
GW806742X is an inhibitor of Mixed Lineage Kinase Domain-Like protein (MLKL) which binds the MLKL pseudokinase domain (Kd: 9.3 μM) with anti-necroptosis activity. GW806742X has activity against VEGFR2.
体外活性
GW806742X (1 μM) retards MLKL translocation to the membrane.GW806742X (0.1-10000 nM) rescues 50% of wild-type mouse dermal fibroblasts (MDFs) from TSQ-induced necroptosis with an IC50< 50 nM when 1 ng/mL TNF is used.
Cas No.
579515-63-2
分子式
C25H22F3N7O4S
分子量
573.55
储存和溶解度
DMSO:125 mg/mL (217.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years