JANEX-1

基本信息

分子式	C16H15N3O3
分子量	297.31
存储条件	Freezer -20℃

半岛bd体育手机客户端 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 ?M）。

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.

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III