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Merck
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Key Documents

539649

Sigma-Aldrich

PKCθ/δ Inhibitor

同義詞:

PKCθ/δ Inhibitor, 5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile

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About This Item

經驗公式(希爾表示法):
C22H18N4O2
分子量::
370.40
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥95% (HPLC)

品質等級

形狀

powder

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

light yellow

溶解度

ethanol: 1 mg/mL
DMSO: 100 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

一般說明

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).

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

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

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 2

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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