| Description |
TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
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| Related Catalog |
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| Target |
IC50: 69 nM (DAPK1), 225 nM (DAPK3)[1]
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| In Vitro |
TC-DAPK 6 is found to be the most potent Death-associated protein kinase (DAPK) inhibitor with enzyme selectivity. When assayed with 10 μM ATP, the IC50 values for DAPK1 and DAPK3 are 69 and 225 nM, respectively. TC-DAPK 6 also inhibits p70S6K (1 μM < IC50< 10 μM)[1].
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| Kinase Assay |
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].
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| 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.
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