TC-DAPK 6 纯度:>95.0% 100mg

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TC-DAPK 6 纯度:>95.0% 100mg

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货号：HY-15513

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商品介绍
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TC-DAPK 6 是一种有效的ATP竞争性的选择性 DAPK 抑制剂，作用于 DAPK1 和 DAPK3，IC₅₀ 分别为 69 和 225 nM。

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).

IC₅₀ & Target

IC50: 69 nM (DAPK1), 225 nM (DAPK3)^[1]

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].

Solvent & Solubility

In Vitro:

DMSO : 18.67 mg/mL (67.57 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

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.

Kinase Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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.

Kinase Assay
^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References