(2R,3S,4S)-2,3-ジヒドロキシ-4-[(メトキシアセチル)アミノ]-5-(3′,5′-ジクロロ-4-ビフェニリル)ペンタン酸

(2R,3S,4S)-2,3-ジヒドロキシ-4-[(メトキシアセチル)アミノ]-5-(3′,5′-ジクロロ-4-ビフェニリル)ペンタン酸 化学特性,用途語,生産方法

• 一般的な説明

  A cell-permeable biphenylylpentanoic acid compound that acts as a selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC₅₀ = 2.5 μM in a Sic1-SCF^Cdc4 assay) without affecting the activities of E1 or E3 ligases. Reported to act by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin-binding site and may serve as a molecular bridge between Cdc34A and ubiquitin. Binds to Cdc34ACAT alone with an EC₅₀ value of 267 μM, but in the presence of ubiquitin, this affinity is significantly increased (EC₅₀ = 19 μM). Does not disrupt the interaction of Cdc34A with the RING domain of Rbx1 and is suggested to even moderately stabilize this interaction. Shown to inhibit p27^Kip1 ubiquitination (IC₅₀ = 1.72 μM) and reduce PC-3 cancer cells proliferation (~30 μM).
  
  Please note that the molecular weight for this compound is batch-specific due to variable water content.

• Biochem/physiol Actions

  Cell permeable: yes

(2R,3S,4S)-2,3-ジヒドロキシ-4-[(メトキシアセチル)アミノ]-5-(3′,5′-ジクロロ-4-ビフェニリル)ペンタン酸 生産企業

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1319207-44-7, (2R,3S,4S)-2,3-ジヒドロキシ-4-[(メトキシアセチル)アミノ]-5-(3′,5′-ジクロロ-4-ビフェニリル)ペンタン酸 キーワード