Koningic acid (Synonyms: (2'S,5aS,6R,9aS)-1,5a,6,7,8,9a-Hexahydro-6-(1-methylethyl)-1-oxo-spiro[2-benzoxepin-9(3H)2'-oxirane]-4-carboxylic acid) |
| カタログ番号GB40253 |
コニン酸（KA; 74310-84-2）は、グリセルアルデヒド-3-リン酸脱水素酵素（GAPDH）の強力で選択的な阻害剤です。阻害は不可逆的であり、活性部位システインがエポキシ基に求核攻撃を行うことによって進行します。ウサギ筋肉GAPDHに対するKi値は1.1μMです。KAは、グルコース依存性ATP枯渇を介して高糖解能がん細胞を選択的に殺すことができます。癌細胞代謝の最も顕著な特徴であるウォーバーグ効果の選択的ターゲティングの予測モデルに使用されています。
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Cas No.: 74310-84-2
Sample solution is provided at 25 µL, 10mM.
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Koningic acid (KA; 74310-84-2) is a potent and selective inhibitor of glyceraldehyde-3-phosphate dehydrogenase (GAPDH). Inhibition is irreversible and proceeds via nucleophilic attack of an active site cysteine on the epoxide moiety, Ki = 1.1 μM for rabbit muscle GAPDH. KA can selectively kill high-glycolytic cancer cells via glucose dependent ATP depletion. Has been used in a predictive model for selective targeting of the Warburg effect, the most prominent hallmark of cancer cell metabolism.
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