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420144 JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem

420144
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
40045-50-9C₅H₃N₅O₂S₃

Products

Catalogue NumberPackaging Qty/Pack
420144-10MG 10 mg
Description
OverviewA cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.
Catalogue Number420144
Brand Family Calbiochem®
Synonyms5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
References
ReferencesDe, S.K., et al. 2009. J. Med. Chem. 52, 1943.
Product Information
CAS number40045-50-9
FormPale yellow solid
Hill FormulaC₅H₃N₅O₂S₃
Chemical formulaC₅H₃N₅O₂S₃
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 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

JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem Certificates of Analysis

TitleLot Number
420144

References

Reference overview
De, S.K., et al. 2009. J. Med. Chem. 52, 1943.
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.

Revision13-April-2011 RFH
Synonyms5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
DescriptionA cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number40045-50-9
Chemical formulaC₅H₃N₅O₂S₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml) or Ethanol (4 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
ReferencesDe, S.K., et al. 2009. J. Med. Chem. 52, 1943.