CAS NO: | 1314118-94-9 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 1314118-94-9 |
别名 | MK 25 |
化学名 | 5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furancarboxamide, monohydrochloride |
Canonical SMILES | O=C(N(C1=CC=C(N2CCNCC2)C=C1)CC3=NC=CC=C3)C4=CC=C(C5=CC=C(Cl)C=C5)O4.Cl |
分子式 | C27H25ClN4O2o HCl |
分子量 | 509.4 |
溶解度 | <5.09mg/mL in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor with IC50 value of 0.11 μM [1]. MAP kinase-activated protein kinase 2 (MAPKAPK2 or MK2) is a member of the Ser/Thr protein kinase family and regulated through direct phosphorylation by p38 MAP kinase. Activation of the p38/MK2 pathway involved in promoting pro-inflammatory cytokine production and related inflammatory diseases [1]. MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor. In a broad panel of 150 protein kinases, MK2 Inhibitor IV only significantly inhibited CK1γ3 at greater than 50%. MK2 Inhibitor IV also demonstrated no inhibition against a panel of cytochrome P450 (CYP) enzymes up to 30 μM. In the human THP1 acute monocytic leukemia cell line, MK2 Inhibitor IV inhibited pro-inflammatory cytokine secretion. MK2 Inhibitor IV also dose-dependently inhibited LPS-stimulated TNFα and IL6 secretion with IC50 values of 4.4 μM and 5.2 μM, respectively. In the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures, MK2 Inhibitor IV dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion with IC50 values of 5.7 μM and 2.2 μM, respectively. Reference: |