N-(4,6-ジメチル-2-ピリジニル)-4-[4-(トリフルオロメチル)ベンジル]ピペラジン-1-カルボチオアミド

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

• 注意書き

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

N-(4,6-ジメチル-2-ピリジニル)-4-[4-(トリフルオロメチル)ベンジル]ピペラジン-1-カルボチオアミド 価格

N-(4,6-ジメチル-2-ピリジニル)-4-[4-(トリフルオロメチル)ベンジル]ピペラジン-1-カルボチオアミド 化学特性,用途語,生産方法

• 説明

  NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC₅₀ value of 2.5 μM. It has been shown to reduce the production of glucose-derived serine in cells and to suppress the growth of PHGDH-dependent MDA-MB-468 cancer cells both in vitro and in mice bearing orthotopic xenograft tumors.

• 使用

  NCT-503 is a novel inhibitor of human Phosphoglycerate Dehydrogenase (PHGDH).

• Biochem/physiol Actions

  NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first, rate-limiting step of glucose-derived serine synthesis. NCT-503 reduced glucose-derived serine production and suppressed the growth of both PHGDH-dependent cancer cells in culture and in xenograft tumors, and caused G1/S cell cycle arrest in MDA-MB-468 cells. NCT-503 reduced the incorporation of one-carbon units from glucose-derived and exogenous serine into nucleotides, which may contribute to its anticancer activity. NCT-503 had an IC50 value of 2.5 μM for PHGDH and was inactive against a panel of other dehydrogenases and minimal cross-reactivity in a panel of 168 G-protein-coupled receptors (GPCRs). NCT-503 was found to be noncompetitive with respect to both 3-PG and NAD+, and exhibit good stability (>98% after 48 hrs in assay buffer) and aqueous solubility.

N-(4,6-ジメチル-2-ピリジニル)-4-[4-(トリフルオロメチル)ベンジル]ピペラジン-1-カルボチオアミド 生産企業

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N-(4,6-ジメチル-2-ピリジニル)-4-[4-(トリフルオロメチル)ベンジル]ピペラジン-1-カルボチオアミド スペクトルデータ(¹HNMR)