MK2 Inhibitor III (compound 16) 是一种具有口服活性、选择性和 ATP 竞争性的 MAPKAP-K2 (MK-2) 抑制剂，IC50 为 0.85 nM。
| Cas No. | 1186648-22-5 |
| Canonical SMILES | O=C(NCC1)C2=C1NC(C3=CC(C4=CC(C=CC=C5)=C5N=C4)=NC=C3)=C2.O |
| 分子式 | C21H16N4O•H2O |
| 分子量 | 358.4 |
| 溶解度 | DMF: 1.4 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml |
| 储存条件 | Store at -20°C |
| 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 | MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation. MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM). It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets. MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM). |
