GPX4-IN-3

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GPX4-IN-3  纯度: 99.69%

GPX4-IN-3 (26a) 是有效的谷胱甘肽过氧化物酶4 (GPX4) 抑制剂，可选择性诱导铁死亡 (ferroptosis)。GPX4-IN-3 (26a) 在1 μM 的浓度可抑制GPX4 71.7% 活性。

GPX4-IN-3

GPX4-IN-3 Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3900 In-stock
10 mg ￥6500 In-stock
25 mg ￥12500 In-stock
50 mg   询价  
100 mg   询价  

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GPX4-IN-3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library

生物活性

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM[1].

体外研究
(In Vitro)

GPX4-IN-3 (26a) exhibits IC50 values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively[1].
GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3[1].
GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity[1].
GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity[1].
GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse 4T1 xenograft model[1].
Dosage: 15 and 30 mg/kg.
Administration: Intravenous injection, every two days for a total of five times.
Result: Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively.

分子量

530.04

Formula

C29H24ClN3O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 67.5 mg/mL (127.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8867 mL 9.4333 mL 18.8665 mL
5 mM 0.3773 mL 1.8867 mL 3.7733 mL
10 mM 0.1887 mL 0.9433 mL 1.8867 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 6.75 mg/mL (12.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 6.75 mg/mL (12.73 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 67.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 6.75 mg/mL (12.73 mM); Clear solution

    此方案可获得 ≥ 6.75 mg/mL (12.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 67.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Congjun Xu, et al. Discovery of a Potent Glutathione Peroxidase 4 Inhibitor as a Selective Ferroptosis Inducer. J Med Chem. 2021 Sep 23;64(18):13312-13326.

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