产品描述

JANEX-1是JAK3小分子抑制剂，选择性抑制JAK3，IC50为78 μM。它不影响JAK1或JAK2，及其他蛋白酪氨酸激酶的活性（IC50 ≥ 350 µM）。

靶点（IC50 & Targe）

JAK3,Ki:2.3μM

体外研究

JANEX-1 inhibits JAK3 but not JAK1 or JAK2. The ZAP/SYK family tyrosine kinase SYK, TEC family tyrosine kinase Bruton’s tyrosine kinase (BTK), SRC family tyrosine kinase LYN, and receptor family tyrosine kinase insulin receptor kinase (IRK) are not inhibited by JANEX-1[1]. JANEX-1 suppresses IL-1β and IFN-γ-induced phosphorylation of STAT-1, STAT-3, and STAT-5 proteins. JANEX-1 has a potent inhibitory effect on cytokine-induced β-cell damage[2].

体内研究

JANEX-1 is very well tolerated by mice and monkeys and effective plasma concentrations of JANEX-1 could be achieved at nontoxic dose levels. JANEX-1 suppresses the mitogen and antigen responses of T-cells and attenuates the severity of T-cell-dependent graft-versus-host disease in a bone marrow transplantation model[1].

动物实验

Animal Models: Female NOD mice

Formulation: DMSO in PBS

Dosages: 20, 50 and 100 mg/kg/day

Administration: IP

(Only for Reference)

参考文献

[1] Cetkovic-Cvrlje M, et al. Clin Immunol. 2003, 106(3):213-25.

[2] Lv N, et al. Exp Cell Res. 2009, 315(12):2064-71.