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405273 INDY - Calbiochem

405273
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
405273-5MG Glass bottle 5 mg
Description
OverviewA 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.
Catalogue Number405273
Brand Family Calbiochem®
SynonymsDyrk/Clk Dual Inhibitor, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone
References
ReferencesOgawa, Y., et al. 2010. Nat Commun 1, 1.
Product Information
FormOff-white powder
Hill FormulaC₁₂H₁₃NO₂S
Chemical formulaC₁₂H₁₃NO₂S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

INDY - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

INDY - Calbiochem Certificates of Analysis

TitleLot Number
405273

References

Reference overview
Ogawa, Y., et al. 2010. Nat Commun 1, 1.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision28-March-2013 JSW
SynonymsDyrk/Clk Dual Inhibitor, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone
DescriptionA 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.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₂H₁₃NO₂S
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesOgawa, Y., et al. 2010. Nat Commun 1, 1.