MK2-IN-3
目录号: PL06954 纯度: ≥98%
CAS No. :724711-21-1
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中文名称
MK2-IN-3
中文别名
2-2-(3-喹啉)-4-吡啶-1,5,6,7-四氢吡咯并[3,2-c]吡啶-4-酮
英文名称
MK2-IN-3
英文别名
2-[2-(quinolin-3-yl)pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one;MK2 Inhibitor III;2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one;MK2-IN-3
Cas No.
724711-21-1
分子式
C21H16N4O
分子量
340.38
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
MK2-IN-3 是一种有效和选择性的 MAPKAP-K2 (MK-2) 抑制剂,IC50 值为 8.5 nM。MK2-IN-3 对 MK-3,MK-5,ERK2,MNK1,p38a (IC50=0.21, 0.081, 3.44, 5.7, >100 μM) 和 MSK1,MSK2,CDK2,JNK2,IKK2 (IC50>200 μM) 表现出良好的选择性。MK2-IN-3 可以减少 U937 细胞和体内 TNFα 的产生。
生物活性
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC 50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC 50 s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC 50 s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo.
性状
Solid
IC50 & Target[1][2]
IC50: 8.5 nM (MK-2); 81 nM (MK-5); 210 nM (MK-3); 3.44 μM (ERK2); 5.7 μM (MNK1)
体外研究(In Vitro)
MK2-IN-3 (compound 16) inhibits MK-2 and TNFα production in U937 cells, with IC50s of 8.5 nM and 4.4 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
MK2-IN-3 (compound 16) (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Anderson DR, et, al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (183.62 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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