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MK2-IN-3

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Chemical Structure| 724711-21-1 同义名 : MK2 Inhibitor III
CAS号 : 724711-21-1
货号 : A950511
分子式 : C21H16N4O
纯度 : 99%+
分子量 : 340.378
MDL号 : MFCD16293712
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(176.27 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
动物实验配方：
生物活性
描述 MAPK-activated protein kinase 2 (MK2), a major effector of the p38 MAPK stress and DNA damage response signaling pathway, and a critical regulator of pro-inflammatory cytokine production, has been identified as a key contributor to colon tumorigenesis under conditions of chronic inflammation[2]. MK2 is critical for MCMV-induced production of IL-10, IFN-α2 and 4, IFN-β, IL-6, and TNF-α but not for IFN-γ. The MCMV-induced IL-10 production requires activation of IFNAR1 and is further regulated by MK2 and TTP-dependent stabilization of IL-10 transcripts. MK2(-/-) mice are able to control acute MCMV replication, despite deregulated cytokine production[3]. In cells with impaired p53 activity, DNA damage repair requires the activation of p38MAPK along with MAPKAP kinase 2 (MK2). In HPV-positive cells, phosphorylation of p38 and MK2 proteins was induced along with relocalization to the cytoplasm[4]. In an autochthonous model of non-small-cell lung cancer (NSCLC), we demonstrate that MK2 is responsible for resistance of p53-deficient tumors to cisplatin, indicating synthetic lethality between p53 and MK2 can successfully be exploited for enhanced sensitization of tumors to DNA-damaging chemotherapeutics in vivo[5]. MK2-IN-3 is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.38mL

5.88mL

2.94mL
参考文献

[1]Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54. doi: 10.1021/jm0611004. Epub 2007 May 5. PMID: 17480064.

[2]Lucia Suarez-Lopez,et al. MAPKAP Kinase-2 Drives Expression of Angiogenic Factors by Tumor-Associated Macrophages in a Model of Inflammation-Induced Colon Cancer. Front Immunol.2021 Feb 23;11:607891.

[3]Christian Ehlting,et al. MAPKAP kinase 2 regulates IL-10 expression and prevents formation of intrahepatic myeloid cell aggregates during cytomegalovirus infections. J Hepatol. 2016 Feb;64(2):380-389.

[4]Ayano Satsuka,et al. p38MAPK and MK2 pathways are important for the differentiation-dependent human papillomavirus life cycle. J Virol. 2015 Feb;89(3):1919-24.

[5]Sandra Morandell,et al. A reversible gene-targeting strategy identifies synthetic lethal interactions between MK2 and p53 in the DNA damage response in vivo. Cell Rep. 2013 Nov 27;5(4):868-77.

[6]Gurgis F, Akerfeldt, MC, Heng B , et al. Cytotoxic activity of the MK2 inhibitor CMPD1 in glioblastoma cells is independent of MK2[J]. Cell Death Discovery, 2015, 1:15028.