MK2-IN-1 HCl

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Chemical Structure| 1314118-94-9 同义名 : MK2 Inhibitor IV; MK2-IN-1 hydrochloride; MK2-IN-1; MK 25
CAS号 : 1314118-94-9
货号 : A790720
分子式 : C27H26Cl2N4O2
纯度 : 99%+
分子量 : 509.43
MDL号 : MFCD29472226
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(206.11 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(196.3 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.81mL

1.96mL

0.98mL

19.63mL

3.93mL

1.96mL
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