| CAS NO: | 1314118-94-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 509.4 |
| Cas No. | 1314118-94-9 |
| Formula | C27H25ClN4O2·HCl |
| Synonyms | MK 25 |
| Solubility | insoluble in DMSO; ≥16.5 mg/mL in EtOH with ultrasonic; ≥37.4 mg/mL in H2O |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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:
[1]. Huang X, Shipps GW Jr, Cheng CC, 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.
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