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MilliporeSigma™ Calbiochem™ PKCθ/δ Inhibitor

Catalog No. 5396495MG Shop All MilliporeSigma Products
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53-964-95MG 5 mg
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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 = 70nM) with much reduced potency against other novel PKCs (IC50

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 = 70nM) with much reduced potency against other novel PKCs (IC50 = 0.35, 2.33, and 16.35μM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC50 >50μM) as well as a panel of 18 other commonly studied cellular kinases (IC50 >10μM). 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).
TRUSTED_SUSTAINABILITY

Specifications

Color Light Yellow
Description 95% by HPLC
Molecular Formula C22H18N4O2
Formula Weight 370.4g/mol
Solubility DMSO or EtOH
Content And Storage Protect from light
Form Powder
Quantity 5 mg
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