MK2-IN-1 hydrochloride
规格
Cas Number | 1314118-94-9 |
规格或纯度 | ≥98% |
纯度 | ≥98% |
包装 | 100mg 或 50mg 或 10mg 或 5mg |
产品信息
品牌 | 阿拉丁 |
溶解性 | H2O : ≥ 100 mg/mL (196.30 mM) DMSO : 100 mg/mL (196.30 mM; Need ultrasonic) |
过滤标签 | MAPKAPK2 (MK2),MAPK/ERK Pathway |
储存温度 | 2-8°C储存 |
运输条件 | 冰袋运输 |
生化和生理学机理 | MK2-IN-1 hydrochloride 是一种强效的 MAPKAPK2(MK2) 选择性抑制剂(IC50=0.11 uM),具有非 ATP 竞争性结合模式:MAPKAPK2(MK2) 抑制剂 (nMK2-IN-1 是通过筛选对 |
英文描述 |
MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM Target: MAPKAPK2(MK2) inhibitorMK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 μM, and only CK1γ3 was significantly inhibited at greater than 50%. MK2-IN-1 inhibited pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion. MK2-IN-1 also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures. Of note, given its high degree of selectivity, our data suggest that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology . Form:Solid |