CAS:1314118-94-9MK2-IN-1 hydrochloride

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Synonyms: MK2 Inhibitor HCl

MK2-IN-1 HCl is a non-ATP competitive inhibitor of MAPKAPK2 (MK2) with IC50 of 0.11 μM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1314118-94-9

储存条件

分子式

C27H26Cl2N4O2

运输

蓝冰

分子量

509.43

别名

MK2 Inhibitor HCl

溶解度

DMSO	98.0 mg/mL (192.4 mM)
Water	115.0 mg/mL (225.7 mM)

动物实验配方

生物活性

描述MAPKAP-K2 (MK2), a direct downstream substrate of p38, plays a crucial role in signaling and synthesis of proinflammatory cytokines, such as TNFα, IL-6 and IFNγ. MK2-IN-1 HCl is a potent, selecitve and non-ATP competitive MK2 inhibitor with an IC₅₀ of 0.11 μM^[3]. Consistent with specific MK2 inhibition, MK2-IN-1 HCl inhibited pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion. MK2-IN-1 HCl also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures^[4].
作用机制MK2-IN-1 HCl inhibits MK2 with a non-ATP competitive binding mode^[3].