SU3327 是具有底物竞争性的JNK选择性抑制剂,IC50为 0.7 μM。它还抑制JNK和 JIP 之间的蛋白相互作用,IC50值为 239 nM。
产品描述
SU3327 is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 μM).
体外活性
TNF-α stimulated phosphorylation of c-Jun in HeLa cells inhibited by SU3327 with EC50 of 6.23 μM[1]. SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1[3].
体内活性
In male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice, SU3327 (25 mg/kg; intraperitoneal injection; ) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes[1]. SU3327 has favorable microsomal and plasma stability (T1/2 = 27 min)[1].
Cas No.
40045-50-9
分子式
C5H3N5O2S3
分子量
261.31
储存和溶解度
DMSO:62.5 mg/mL (239.19 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years