TC-DAPK 6
TC-DAPK 6 是一种有效的、ATP 竞争性的、高度选择性的 DAPK 抑制剂（对 DAPK1 和 DAPK3 的 IC50 分别为 69 和 225 nM，ATP 浓度为 10 μM）。
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包装价格促销价数量
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10mg￥762.00610.00- +
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50mg￥2700.002160.00- +
- 货号: ajci12142
- CAS: 315694-89-4
- 别名: DAPK inhibitor
- 分子式: C17H12N2O2
- 分子量: 276.29
- 纯度: >98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Death-associated protein kinase (DAPK) is a serine/threonine protein kinase implicated in diverse programmed cell death pathways. DAPK is a promising target protein for the treatment of ischemic diseases. TC-DAPK 6 is an oxazalone compound that acts as a potent, ATP-competitive, and highly selective death-associated protein kinase (DAPK) inhibitor (IC50 = 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP); while exhibiting much reduced or no activity against a panel of 48 other kinases even at concentrations as high as 10 μM.Protocol
Kinase experiment: | Kinase assay is performed using the Z’-LYTE kinase assay kit Ser/Thr 13 peptide. The standard reaction for compound screening contained 1 mM peptide substrate, 10 mM ATP, 50 mM HEPES (pH 7.4), 10 mM MgCl2, 0.01% Brij-35, and 0.5% DMSO. Human recombinant DAPK1 is used at a final concentration of 2.6 μg/mL, and recombinant DAPK3 is used at a final concentration 1.5 mg/mL. To test the enzyme selectively of the inhibitors (e.g., TC-DAPK 6), ProfilerPro kits are used in the protocol[1]. |
参考文献: [1]. Okamoto M, et al. Identification of death-associated protein kinases inhibitors using structure-based virtual screening. J Med Chem. 2009 Nov 26;52(22):7323-7. | |
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￥2120.00 ￥2650.00
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￥1920.00 ￥2400.00
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