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219511 Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Clk Inhibitor IV, (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate

219511
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₁₃Cl₂N₃O₂
Description
Overview

This product has been discontinued.



A cell-permeable N-methylindolyl-enaminonitrile that acts as a potent inhibitor against CLK1, DYRK1A (IC50 = 19.7 and 55.2 nM, respectively), and likely CLK4, while exhibiting much lower potency against CLK3 (IC50 = 0.53 µM) and little activity toward a panel of 71 other protein kinases. Shown to be more effective than TG003 (Cat. No. 219479) in suppressing both basal and TNF-α-stimulated SRp55 and SRp75 phosphorylation, as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1 (5 to 10 µM).
Catalogue Number219511
Brand Family Calbiochem®
SynonymsClk Inhibitor IV, (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
References
ReferencesFedorov, O., et al. 2011. Chem. Biol. 18, 67.
Product Information
FormWhite solid
Hill FormulaC₁₅H₁₃Cl₂N₃O₂
Chemical formulaC₁₅H₁₃Cl₂N₃O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% 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 at Ambient Temperature or 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
Global Trade Item Number
Catalogue Number GTIN
219511 0

Documentation

Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Cdc2-Like Kinase Inhibitor IV, KH-CB19 - Calbiochem Certificates of Analysis

TitleLot Number
219511

References

Reference overview
Fedorov, O., et al. 2011. Chem. Biol. 18, 67.
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.

Revision16-April-2012 JSW
SynonymsClk Inhibitor IV, (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
DescriptionA cell-permeable N-methylindolyl-enaminonitrile that acts as a more potent inhibitor than TG003 (Cat. No. 219479) against CLK1 activity (IC50 = 19.7 and 48.6 nM, respectively) by targeting the kinase ATP binding site in a non-ATP mimetic fashion. KH-CB19 is also reported to exhibit higher potency than TG003 against DYRK1A (IC50 = 55.2 vs. 156.1 nM, respectively) and CLK3 (IC50 = 0.53 vs. >4 µM, respectively), while exhibiting no activity against a panel of 71 other protein kinases. Thermostability shift assay reveals stronger interaction of KH-CB19 toward CLK4 than CLK1, predicting better or at least comparable potency against CLK4. KH-CB19 is shown to be more effective than TG003 in suppressing both basal and TNF-α-stimulated phosphorylation of serine/arginine rich proteins SRp55 (77.5% vs. 45% inhibition by 5 µM respective inhibitor against stimulated level) and SRp75 (80% vs. 27.5% inhibition by 5 µM respective inhibitor against stimulated level), as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₅H₁₃Cl₂N₃O₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
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
ReferencesFedorov, O., et al. 2011. Chem. Biol. 18, 67.