ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM).
Cas No. | 1049738-54-6 |
Canonical SMILES | CCOC1=CC=C(/C=C2SC(N(CCN)C\2=O)=O)C=C1.Cl |
分子式 | C14H16N2O3S•HCl |
分子量 | 328.8 |
溶解度 | DMSO: 2 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 | ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 µM). This prevents its interaction with protein substrates without inhibiting catalytic activity. ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2. Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC50 = 15-20 µM), A549 lung carcinoma cells (IC50 = 25 µM), Sum-159 estrogen receptor-negative breast cancer cells and HT1080 fibrosarcoma cells. |