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RK-24466 (KIN 001-51) 是高效的、选择性的 Lck 抑制剂,对 Lck (64-509) 和 LckCD 亚型的 IC50 值分别为小于 1 和2 nM。
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RK-24466 (KIN 001-51) 是高效的、选择性的 Lck 抑制剂,对 Lck (64-509) 和 LckCD 亚型的 IC50 值分别为小于 1 和2 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,980 | 现货 | |
25 mg | ¥ 3,520 | 现货 | |
50 mg | ¥ 4,920 | 现货 | |
100 mg | ¥ 6,930 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,360 | 现货 |
产品描述 | RK-24466 (KIN 001-51) is a selective and potent inhibitor of Lck, inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively. |
靶点活性 | Lck (64-509):<1 nM (IC50), LckCD:2 nM (IC50) |
体外活性 | RK-24466, a lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, significantly inhibited both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreased the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb). Additionally, RK-24466 suppressed the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury. The present study identified RK-24466 as a potent VSMC proliferation and migration inhibitor and warrants further studies to elucidate its more detailed molecular mechanisms, such as its primary target, and to further validate its in vivo efficacy as a therapeutic agent for pathologic vascular conditions, such as restenosis and atherosclerosis[1]. |
别名 | KIN 001-51 |
分子量 | 370.45 |
分子式 | C23H22N4O |
CAS No. | 213743-31-8 |
Smiles | Nc1ncnc2n(cc(-c3ccc(Oc4ccccc4)cc3)c12)C1CCCC1 |
密度 | 1.3g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 40 mg/mL (107.97 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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