您好,欢迎来到半岛电竞官方网址 ! [ 登录] [ 免费注册]
半岛电竞官方网址
位置: 首页> 半岛bd体育手机客户端 库> JH-X-119-01
立即咨询
咨询类型:
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
JH-X-119-01
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JH-X-119-01图片
CAS NO: 2227368-54-7
包装与价格:
包装 价格(元)
5mg 电议
10mg 电议
25mg 电议
50mg 电议
100mg 电议

半岛bd体育手机客户端 介绍
JH-X-119-01 是一种有效的选择性白介素 1 受体相关激酶 1 (IRAK1) 抑制剂。JH-X-119-01 可改善 LPS 诱导的小鼠败血症。JH-X-119-01 抑制 IRAK1,IC50 为 9 nM,而在浓度高达 10 μM 时对 IRAK4 也没有抑制作用。
Cas No. 2227368-54-7
分子式 C25H20N6O3
分子量 452.46
溶解度 DMSO : 250 mg/mL (552.54 mM; Need ultrasonic)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM[2].

JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation[1].JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4[2].JH-X-119-01 shows moderate cell killing effects in a panel of Waldenstr?m’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 μM[2].

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg[1].

[1]. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597.
[2]. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243.

Baidu
map