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。
货号:ajcx32516
CAS:724711-21-1
分子式:C21H16N4O
分子量：340.38
溶解度:DMSO : 62.5 mg/mL (183.62 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

参考文献:
[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.