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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
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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assay

≥95% (HPLC)

Quality Segment

100

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

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

Deleterious substance

pdsc

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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