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CAS No.: 1314118-94-9

MK2-IN-1 HCl Catalog No. CSN17687

Synonyms: MK2 Inhibitor IV;MK 25;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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技术信息

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].
参考文献

[1] Rao AU, Xiao D, et al. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72.
[2] Huang X, Zhu X, et al. A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70.
[3] Rao AU, Xiao D, Huang X, et al. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett. 2012;22(2):1068-1072
[4] 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;2(8):632-637

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9630 mL
- 9.8149 mL
- 19.6298 mL
- 5 mM
- 0.3926 mL
- 1.9630 mL
- 3.9260 mL
- 10 mM
- 0.1963 mL
- 0.9815 mL
- 1.9630 mL

技术信息

CAS号

1314118-94-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H26Cl2N4O2

运输

蓝冰

分子量

509.43

别名

MK2 Inhibitor IV;MK 25;MK2 Inhibitor HCl

溶解度

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

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