Elesclomol伊利司莫,488832-69-5

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Elesclomol

CAS No. : 488832-69-5

MCE 国际站：Elesclomol

产品活性：Elesclomol (STA-4783) 是一种有效的铜离子载体，可促进铜死亡 (cuproptosis)。Elesclomol 特异性结合铁氧还蛋白 1 (FDX1) α2/α3 螺旋和 β5 链，抑制 FDX1 介导的 Fe-S 簇生物合成。Elesclomol 是一种氧化应激诱导剂，可诱导癌细胞凋亡。Elesclomol 是一种活性氧 (ROS) 诱导剂。Elesclomol 可用于 Menkes 和相关的遗传性铜缺乏症研究。

研究领域：Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB  |  Apoptosis

作用靶点：Reactive Oxygen Species  |  Apoptosis

In Vitro: Elesclomol (STA-4783) binds the FDX1 α2/α3 helices and β5 strand, but does not bind the paralog protein FDX2. Elesclomol-Cu(II) is an FDX1 neo-substrate. FDX1 protein binds and reduces the elesclomol-Cu(II) complex.
Elesclomol-Cu (1:1 ratio) (40 nM) for only 2 hours results in a 15- to 60-fold increase in intracellular copper levels that triggered cell death more than 24 hours later in ABC1 cells.
The addition of copper to elesclomol at a 1:1 molar ratio prior to treatment significantly reduces cell viability when cells are grown in glycolytic (glucose media) conditions.
Elesclomol (200 nM; 18 hours) treatment increases the number of early and late apoptotic cells in HSB2 cells. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress.
Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 cells with IC₅₀ values of 110 nM, 24 nM and 9 nM, respectively.

In Vivo: Elesclomol (10 mg/kg; subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54) treatment ameliorates severe cardiac pathology with a partial reduction in hypertrophy. Cardiac [Cu] increased with Elesclomol treatment from a vehicle knockout level of 34 to 55%.
Elesclomol escorted copper to the mitochondria and increased cytochrome c oxidase levels in the brain. Elesclomol prevents detrimental neurodegenerative changes and improved the survival of the mottled-brindled mouse.

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