Description
IQ-1S (1421610-21-0) is a JNK3 inhibitor (Kd = 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively). Displays anti-inflammatory and immunosuppressive activity. Inhibits LPS-induced proinflammatory cytokine and nitric oxide release?in vitro.1?Attenuates collagen-induced arthritis severity and inhibits murine delayed-type hypersensitivity?in vivo.2
Uses
IQ 1S is a JNK inhibitor which inhibits LPS-induced proinflammatory.
in vivo
When mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1) i.p., the serum exposure of the compound is also good, with AUC0-12h values of 2.9 and 7.4 μM/h, respectively[1].
IC 50
JNK3: 87 nM (Kd); JNK2: 360 nM (Kd); JNK1: 390 nM (Kd); PI3Kγ: 1.2 μM (Kd); CK1δ: 1.4 μM (Kd); MKNK2: 1.8 μM (Kd)
References
1) Schepetkin?et al.?(2012),?Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors; Mol. Pharmacol.,?81?832
2) Schepetkin?et al.?(2015),?Anti-Inflammatory effects and Joint Protection in Collagen-Induced Arthritis after Treatment with IQ-1A, a Selective c-Jun N-Terminal Kinase Inhibitor; J. Pharmacol. Exp. Ther.,?353?505
