MK-2 Inhibitor III
Cat. No.：YN350083
| 产品名称: | MK-2 Inhibitor III |
| CAS No.: | 1186648-22-5 |
| Chemical Name: | 1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one, monohydrate |
| Synonyms: | MK-2 Inhibitor III |
| 分子量: | 358.39 |
| 分子式: | C₂₁H₁₈N₄O₂ |
| SMILES: | O=C1C2=C(NC(C3=CC(C4=CC5=CC=CC=C5N=C4)=NC=C3)=C2)CCN1.O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | MK-2 Inhibitor III (compound 16) 是一种具有口服活性的，选择性的，ATP 竞争性的MAPKAP-K2 (MK-2)抑制剂，IC50值为 0.85 nM，MK-2 Inhibitor III 对 MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) 以及 CDK2, JNK2, IKK2, MSK1, and MSK2 也具有选择性。 |
| IC50和靶点: | |
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| Solvent & Solubility: |
Huang, X., Shipps, G.W., Jr., Cheng, C.C., et al.Discovery and hit-to-lead optimization of non-ATP competitive MK2 (MAPKAPK2) inhibitorsACS Med. Chem. Lett.2(8),632-637(2011)
Wang, X., Khaleque, M.A., Zhao, M.J., et al.Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 bindingJ. Biol. Chem.281(2),782-791(2006)
Werz, O., Szellas, D., Steinhilber, D., et al.Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2)J. Biol. Chem.277(17),14793-14800(2002)
Anderson, D.R., Meyers, M.J., Vernier, W.F., et al.Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)J. Med. Chem.50(11),2647-2654(2007)
