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CAS No.: 502887-71-0

MMP-9-IN-1 Catalog No. CSN25314

Synonyms: OUN87710

MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor that selectively targets the hemopexin (PEX) domain of MMP-9.

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靶点选择性

生物活性

实验方案

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^[1]. 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^[2].
作用机制MK2-IN-1 HCl inhibits MK2 with a non-ATP competitive binding mode^[1].
参考文献

[1] 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
[2] 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
- 2.7072 mL
- 13.5360 mL
- 27.0719 mL
- 5 mM
- 0.5414 mL
- 2.7072 mL
- 5.4144 mL
- 10 mM
- 0.2707 mL
- 1.3536 mL
- 2.7072 mL

技术信息

CAS号

502887-71-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H17F2N3O3S

运输

蓝冰

分子量

369.39

别名

OUN87710

溶解度

DMSO	74.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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