405273

Sigma-Aldrich

INDY - Calbiochem

Synonym(s):
INDY - Calbiochem, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone, Dyrk/Clk Dual Inhibitor
Empirical Formula (Hill Notation):
C12H13NO2S
Molecular Weight:
235.30
Pricing and availability is not currently available.

storage conditions

-20C

Quality Level

assay

≥98% (HPLC)

form

powder

mfr. no.

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

wet ice

General description

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.

Packaging

5 mg in Glass bottle
Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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