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INDY-Calbiochem
产品别名
INDY-Calbiochem
(1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone, Dyrk/Clk Dual Inhibitor
基本信息
| Empirical Formula【经验(实验)分子式】 | C12H13NO2S |
| Molecular weight | 235.30 |
| General description【一般描述】 | A benzothiazole compound that acts as an ATP competitive Dyrk inhibitor (IC50 = 0.24 µM and 0.23 µM for Dyrk1A and Dyrk1B, respectively), and displays >90% inhibition on DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D), and PIM1 among a panel of 66 kinases, in an in vitro screening assay. Unlike harmine, another potent Dyrk inhibitor, this compound does not affect MAOA activity. It is shown to decrease substrate phosphorylation of tau-protein at Thr212 in COS7 cells, dose-dependently, from 3 µM to 30 µM and ameliorates the inhibitory effect of Dyrk1A on NFAT response element mediated calcineurin/NFAT signaling in HEK293 cells. In addition, its prodrug, proINDY is shown to effectively reverse developmental defects associated with Dyrk1A overexpression in a Xenopus embryo model at 2.5 µM in vivo, without apparent toxicity. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Other Notes【其他说明】 | Ogawa, Y., et al. 2010. Nat Commun1, 1. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| shipped in【运输】 | wet ice |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | 5 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
