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MK2 Inhibitor IV
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 Inhibitor IV图片
CAS NO:1314118-94-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
MK2 Inhibitor IV 是一种有效且选择性的 MAPKAPK2(MK2) 抑制剂 (IC50=0.11 uM),具有非 ATP 竞争性结合模式。
Cas No.1314118-94-9
别名MK 25
化学名5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furancarboxamide, monohydrochloride
Canonical SMILESO=C(N(C1=CC=C(N2CCNCC2)C=C1)CC3=NC=CC=C3)C4=CC=C(C5=CC=C(Cl)C=C5)O4.Cl
分子式C27H25ClN4O2o HCl
分子量509.4
溶解度<5.09mg/mL in DMSO
储存条件Store at -20℃
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 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor with IC50 value of 0.11 μM [1].

MAP kinase-activated protein kinase 2 (MAPKAPK2 or MK2) is a member of the Ser/Thr protein kinase family and regulated through direct phosphorylation by p38 MAP kinase. Activation of the p38/MK2 pathway involved in promoting pro-inflammatory cytokine production and related inflammatory diseases [1].

MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor. In a broad panel of 150 protein kinases, MK2 Inhibitor IV only significantly inhibited CK1γ3 at greater than 50%. MK2 Inhibitor IV also demonstrated no inhibition against a panel of cytochrome P450 (CYP) enzymes up to 30 μM. In the human THP1 acute monocytic leukemia cell line, MK2 Inhibitor IV inhibited pro-inflammatory cytokine secretion. MK2 Inhibitor IV also dose-dependently inhibited LPS-stimulated TNFα and IL6 secretion with IC50 values of 4.4 μM and 5.2 μM, respectively. In the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures, MK2 Inhibitor IV dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion with IC50 values of 5.7 μM and 2.2 μM, respectively.

Reference:
[1].  Huang X, Shipps GW Jr, Cheng CC, et al. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. ACS Med Chem Lett. 2011 Jun 24;2(8):632-7.