Product Information
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

Documentation

PKCθ/δ Inhibitor SDS

Title

Safety Data Sheet (SDS) 

PKCθ/δ Inhibitor Certificates of Analysis

TitleLot Number
539649

References

Reference overview
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 +2°C to +8°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
ReferencesCole, D.C., et al. 2008. J. Med. Chem. 51, 5958.

Related Products & Applications

Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Kinase C (PKC) Inhibitors