539649
PKCθ/δ Inhibitor
Synonym(s):
PKCθ/δ Inhibitor, 5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
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About This Item
Empirical Formula (Hill Notation):
C22H18N4O2
Molecular Weight:
370.40
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
assay
≥95% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
ethanol: 1 mg/mL
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A 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).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Cole, D.C., et al. 2008. J. Med. Chem.51, 5958.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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