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MK2-IN-1 HCl {[allProObj[0].p_purity_real_show]}

货号:A790720 同义名: MK2 Inhibitor IV; MK2-IN-1 hydrochloride

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

MK2-IN-1 HCl 化学结构 CAS号:1314118-94-9
MK2-IN-1 HCl 化学结构
CAS号:1314118-94-9
MK2-IN-1 HCl 3D分子结构
CAS号:1314118-94-9
MK2-IN-1 HCl 化学结构 CAS号:1314118-94-9
MK2-IN-1 HCl 3D分子结构 CAS号:1314118-94-9
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MK2-IN-1 HCl 纯度/质量文件 产品仅供科研

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MK2-IN-1 HCl 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].

MK2-IN-1 HCl 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

MK2-IN-1 HCl 实验方案

计算器
存储液制备 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

MK2-IN-1 HCl 技术信息

CAS号1314118-94-9
分子式C27H26Cl2N4O2
分子量 509.43
SMILES Code O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5.[H]Cl
MDL No. MFCD29472226
别名 MK2 Inhibitor IV; MK2-IN-1 hydrochloride; MK2-IN-1; MK 25
运输蓝冰
InChI Key AZDOSXSDARWKGX-UHFFFAOYSA-N
Pubchem ID 70681199
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案

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)

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