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TC-DAPK 6 Sale

(Synonyms: DAPK inhibitor) 目录号 : GC13950

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)。

TC-DAPK 6 Chemical Structure

Cas No.:315694-89-4

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10mg
¥630.00
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50mg
¥2,237.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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].

References:

[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.

化学性质

Cas No. 315694-89-4 SDF
别名 DAPK inhibitor
化学名 (4E)-2-[(E)-2-phenylethenyl]-4-(pyridin-3-ylmethylidene)-1,3-oxazol-5-one
Canonical SMILES C1=CC=C(C=C1)C=CC2=NC(=CC3=CN=CC=C3)C(=O)O2
分子式 C17H12N2O2 分子量 276.29
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.6194 mL 18.0969 mL 36.1939 mL
5 mM 0.7239 mL 3.6194 mL 7.2388 mL
10 mM 0.3619 mL 1.8097 mL 3.6194 mL
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