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Merck
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Key Documents

405273

Sigma-Aldrich

INDY

同義詞:

INDY, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone, Dyrk/Clk Dual Inhibitor

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About This Item

經驗公式(希爾表示法):
C12H13NO2S
CAS號碼:
分子量::
235.30
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

品質等級

形狀

powder

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

off-white

溶解度

DMSO: 50 mg/mL

運輸包裝

wet ice

儲存溫度

−20°C

一般說明

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.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

Ogawa, Y., et al. 2010. Nat Commun1, 1.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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