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JANEX-1

品牌
J&K
CAS
202475-60-3
货号
1563401
规格纯度
98%, 一种有效的特异性 JAK3 抑制剂
参考价格
902 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
202475-60-3
JANEX-1
WHI-P131; Jak3 inhibitor I
产品介绍:

基本信息

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

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.

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

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