ASK1-IN-1 是一种凋亡信号调节激酶 1(SK1) 抑制剂,具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。
产品描述
ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.
体外活性
ASK1-IN-1 shows good potency with cell IC50 of 138 nM. ASK1-IN-1 has superior CYP inhibition profile[1].
体内活性
ASK1-IN-1 shows low clearance (rat Cl/Clu = 0.36/6.7 L h-1 kg-1) and good CNS penetration (rat K p,uu = 0.38). ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC50/IC70/IC90 at trough in the brain for 12 hours of 50/115/435 mg/kg respectively[1].
Cas No.
2411382-24-4
储存和溶解度
DMF:4 mg/mL (9.87 mM),Need ultrasonic
Ethanol:< 1 mg/mL (insoluble)
DMSO:< 1 mg/mL (insoluble or slightly soluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years