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MK2-IN-1 (MK2 Inhibitor) Sale

目录号 : GC33142

MK2-IN-1 (MK2 Inhibitor) 是一种有效的、选择性的 MAPKAPK2(MK2) 抑制剂 (IC50=0.11 uM),具有非 ATP 竞争性结合模式。

MK2-IN-1 (MK2 Inhibitor) Chemical Structure

Cas No.:1314118-92-7

规格 价格 库存 购买数量
2mg
¥803.00
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5mg
¥1,696.00
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10mg
¥3,035.00
现货
50mg
¥13,388.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM [1]Target: MAPKAPK2(MK2) inhibitorMK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 μM, and only CK1γ3 was significantly inhibited at greater than 50%. MK2-IN-1 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 also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures. Of note, given its high degree of selectivity, our data suggest that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology [3].

[1]. Rao AU, 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, 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]. Huang X, et al. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. ACS Med Chem Lett. 2011 Jun 24;2(8):632-7.

化学性质

Cas No. 1314118-92-7 SDF
Canonical SMILES O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5
分子式 C27H25ClN4O2 分子量 472.97
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1143 mL 10.5715 mL 21.143 mL
5 mM 0.4229 mL 2.1143 mL 4.2286 mL
10 mM 0.2114 mL 1.0571 mL 2.1143 mL
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