CAS號(hào)	488832-69-5	產(chǎn)地	國(guó)產(chǎn)
規(guī)格	5mg	級(jí)別	化工級(jí)
證書(shū)	ISO系列證書(shū)

Elesclomol (Synonyms: 伊利司莫; STA-4783)

Elesclomol (STA-4783) 是一種有效的銅離子載體，可促進(jìn)銅死亡 (cuproptosis)。Elesclomol 特異性結(jié)合鐵氧還蛋白 1 (FDX1) α2/α3 螺旋和 β5 鏈，抑制 FDX1 介導(dǎo)的 Fe-S 簇生物合成。Elesclomol 是一種氧化應(yīng)激誘導(dǎo)劑，可誘導(dǎo)ai細(xì)胞凋亡。Elesclomol 是一種活性氧 (ROS) 誘導(dǎo)劑。Elesclomol 可用于 Menkes 和相關(guān)的遺傳性銅缺乏癥研究。

生物活性

Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research^[1]^[2]^[3]^[4].

體外研究(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^[1].
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^[1].
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^[2].
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^[3].
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^[5].

Apoptosis Analysis^[3]

Cell Line:	HSB2 cells
Concentration:	200 nM
Incubation Time:	18 hours
Result:	Increased the number of early and late apoptotic cells.

體內(nèi)研究(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%^[4].
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^[4].

Animal Model:	Cardiac Ctr1 knockout mice^[4]
Dosage:	10 mg/kg
Administration:	Subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54
Result:	Ameliorated severe cardiac pathology with a partial reduction in hypertrophy.

分子量：400.52

Formula：C₁₉H₂₀N₄O₂S₂

CAS 號(hào)：488832-69-5

中文名稱：伊利司莫

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 100 mg/mL (249.68 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.4968 mL	12.4838 mL	24.9675 mL
5 mM	0.4994 mL	2.4968 mL	4.9935 mL
10 mM	0.2497 mL	1.2484 mL	2.4968 mL

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution
2.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

參考文獻(xiàn)

[1]. Peter Tsvetkov, et al. Copper induces cell death by targeting lipoylated TCA cycle proteins. Science. 2022 Mar 18;375(6586):1254-1261.

[2]. Peter Tsvetkov, et al. Mitochondrial metabolism promotes adaptation to proteotoxic stress. Nat Chem Biol. 2019 Jul;15(7):681-689.

[3]. Kirshner JR, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27.

[4]. Liam M Guthrie, et al. Elesclomol alleviates Menkes pathology and mortality by escorting Cu to cuproenzymes in mice. Science. 2020 May 8;368(6491):620-625.

[5]. Bair JS, et al. Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. J Am Chem Soc. 2010 Apr 21;132(15):5469-7

注：產(chǎn)品僅用于科研