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CAS No.: 315694-89-4

TC-DAPK 6 Catalog No. CSN16624

Synonyms: DAPK Inhibitor;T-6908224

TC-DAPK 6 is an oxazalone compound that acts as a potent, ATP-competitive, and is a highly selective death-associated protein kinase (DAPK) inhibitor (IC50 = 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).

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描述Death-associated protein kinases (DAPKs) play a central role in programmed cell death such as apoptosis and autophagy and are now emerging as targets for drug discovery in novel therapeutic approaches for ischemic diseases in the brain, heart, kidney, and other organs. TC-DAPK 6 is a potent, selective and ATP-competitive DAPKs inhibitor, acting on DAPK1 and DAPK3 with IC₅₀s of 69 and 225 nM, respectively. In a kinase panel assay, TC-DAPK 6 exhibited much reduced or no activity against a panel of other 48 serine/threonine- or tyrosine-kinases tested to date. TC-DAPK 6 also inhibited P70S6K with an IC₅₀ of 1μM^[2].
作用机制TC-DAPK 6 possesses the additional hydrophobic interaction in the ATP binding cavity of DAPK^[2].
参考文献

[1] Okamoto M, Takayama K, et al. Identification of death-associated protein kinases inhibitors using structure-based virtual screening. J Med Chem. 2009 Nov 26;52(22):7323-7.
[2] Okamoto M, Takayama K, Shimizu T, Ishida K, Takahashi O, Furuya T. Identification of death-associated protein kinases inhibitors using structure-based virtual screening. J Med Chem. 2009 Nov 26;52(22):7323-7

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6194 mL
- 18.0970 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

技术信息

CAS号

315694-89-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12N2O2

运输

蓝冰

分子量

276.29

别名

DAPK Inhibitor;T-6908224

溶解度

DMSO	18.67 mg/mL (67.6 mM)
Water	Insoluble

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