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MK2-IN-3
本产品不向个人销售,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。
MK2-IN-3图片
CAS NO:724711-21-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MK2-IN-3 是一种有效和选择性的 MAPKAP-K2 (MK-2) 抑制剂,IC50 值为 8.5 nM。MK2-IN-3 对 MK-3,MK-5,ERK2,MNK1,p38a (IC50=0.21, 0.081, 3.44, 5.7, >100 µM) 和 MSK1,MSK2,CDK2,JNK2,IKK2 (IC50>200 µM) 表现出良好的选择性。MK2-IN-3 可以减少 U937 细胞和体内 TNFα 的产生。
Cas No.724711-21-1
Canonical SMILESO=C1C2=C(NC(C3=CC(C4=CC5=CC=CC=C5N=C4)=NC=C3)=C2)CCN1
分子式C21H16N4O
分子量340.38
溶解度DMSO : 62.5 mg/mL (183.62 mM)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 µM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 µM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo[1].

MK2-IN-3 (compound 16) inhibits MK-2 and TNFα production in U937 cells, with IC50s of 8.5 nM and 4.4 µM, respectively[1].

MK2-IN-3 (compound 16) (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model[1].

References:
[1]. Anderson DR, et, al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.