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539649 PKCθ/δ Inhibitor

539649
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₂₂H₁₈N₄O₂

Products

KatalógusszámCsomagolás Menny./csomag
539649-5MG Üvegpalack 5 mg
Description
OverviewA cell-permeable pyridinecarbonitrile compound that acts as a potent, ATP-competitive (Ki = 79 nM, using PKCθ KD in coupled PK/LDH assays), and isozyme-selective PKCθ inhibitor (IC50 = 70 nM) with much reduced potency against other novel PKCs (IC50 = 0.35, 2.33, and 16.35 µM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC50 >50 µM) as well as a panel of 18 other commonly studied cellular kinases (IC50 >10 µM). Shown to preferentially inhibit IL-2 production from anti-CD3- and anti-CD28-activated T cells derived from wild-type over PKCθ-knockout mice (IC50 = 58 and 231 nM, respectively).
Catalogue Number539649
Brand Family Calbiochem®
Synonyms5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
References
ReferencesCole, D.C., et al. 2008. J. Med. Chem. 51, 5958.
Product Information
FormLight yellow powder
Hill FormulaC₂₂H₁₈N₄O₂
Chemical formulaC₂₂H₁₈N₄O₂
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 Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°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
Katalógusszám GTIN
539649-5MG 04055977194845

Documentation

PKCθ/δ Inhibitor MSDS

Title

Safety Data Sheet (SDS) 

PKCθ/δ Inhibitor Certificates of Analysis

TitleLot Number
539649

References

Hivatkozások áttekintése
Cole, D.C., et al. 2008. J. Med. Chem. 51, 5958.
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.

Revision21-March-2011 RFH
Synonyms5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
DescriptionA cell-permeable pyridinecarbonitrile compound that acts as a potent, ATP-competitive (Ki = 79 nM, using PKCθ KD in coupled PK/LDH assays), and isozyme-selective PKCθ inhibitor (IC50 = 70 nM) with much reduced potency against other novel PKCs (IC50 = 0.35, 2.33, and 16.35 µM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC50 >50 µM) as well as a panel of 18 other commonly studied cellular kinases (IC50 >10 µM). Shown to preferentially inhibit IL-2 production from anti-CD3- and anti-CD28-activated T cells derived from wild-type over PKCθ-knockout mice (IC50 = 58 and 231 nM, respectively).
FormLight yellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₂H₁₈N₄O₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (1 mg/ml)
Storage Protect from light
+2°C to +8°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
ReferencesCole, D.C., et al. 2008. J. Med. Chem. 51, 5958.