2. Apoptosis
  3. Ferroptosis
  4. Ferroptosis-IN-22

Ferroptosis-IN-22 是一种选择性铁死亡 (ferroptosis) 抑制剂，由 NCOA4 并破坏其与铁蛋白的相互作用介导，其 EC50 为 520 nM，Kd 值为 0.78 μM。Ferroptosis-IN-22 对多种铁死亡诱导剂 (RSL3 (HY-100218A)、Erastin (HY-15763)、ML210 (HY-100003)、FIN56 (HY-103087)) 诱导的铁死亡具有强抑制活性，但不能抑制 H2O2 诱导的细胞坏死或 STS (HY-15141) 诱导的细胞凋亡。Ferroptosis-IN-22 可有效改善 Concanavalin A (HY-P2149) 诱导的急性肝损伤。Ferroptosis-IN-22 可用于研究铁死亡相关疾病。

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Ferroptosis-IN-22

Ferroptosis-IN-22 Chemical Structure

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Ferroptosis-IN-22 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ferroptosis-IN-22 is a selective ferroptosis inhibitor by targeting NCOA4 and disrupting its interaction with ferritin with an EC50 of 520 nM and a Kd of 0.78 μM. Ferroptosis-IN-22 has a strong inhibitory activity against ferroptosis induced by multiple ferroptosis inducers (RSL3 (HY-100218A), Erastin (HY-15763), ML210 (HY-100003), FIN56 (HY-103087)), but does not inhibit necrosis induced by H2O2 or apoptosis induced by STS (HY-15141). Ferroptosis-IN-22 effectively ameliorates Concanavalin A (HY-P2149)-induced acute liver injury. Ferroptosis-IN-22 can be used for the study of ferroptosis-related diseases[1].

体外研究
(In Vitro)

Ferroptosis-IN-22 (Compound 4k) 表现出抗铁死亡活性，在 HT-1080 细胞中 EC50 值分别为 0.515 μM (RSL3) 和 2.776 μM (Erastin) ，在 786-O 细胞中 EC50 值分别为 0.4061 μM (RSL3) 和 1.308 μM (Erastin) ，在 MDA-MB-231 细胞中 EC50 值分别为 0.093 μM (RSL3) 和 1.013 μM (Erastin) ，并且还能抑制 ML210 和 FIN56 诱导的铁死亡[1]。
Ferroptosis-IN-22 (4-8 μM) 显著降低 RSL3 或 Erastin 诱导的 HT-1080 和 786-O 细胞中的脂质过氧化，并且不具有直接的抗氧化活性[1]。
Ferroptosis-IN-22 (4 μM，6 小时) 直接与铁蛋白自噬中的关键受体蛋白 NCOA4 结合，破坏 NCOA4 与铁蛋白 (FTH1) 之间的相互作用，从而抑制 HT-1080 细胞中的铁蛋白自噬过程，而不是依赖于直接的铁螯合[1]。
Ferroptosis-IN-22 表现出低心脏毒性和极低的 CYP 介导的药物相互作用 (DDI) 风险[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ferroptosis-IN-22 相关抗体:

Western Blot Analysis[1]

Cell Line: HT-1080 cells
Concentration: 4 μM
Incubation Time: 6 h
Result: Significantly reduced the amount of FTH1/FTL co-precipitated with NCOA4.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 10 mg/kg p.o. T1/2 3.751 h
Rat 5 mg/kg i.v. T1/2 4.009 h
Rat 10 mg/kg p.o. Tmax 2.000 h
Rat 5 mg/kg i.v. Tmax 0.083 h
Rat 10 mg/kg p.o. Cmax 557.082 ng/mL
Rat 5 mg/kg i.v. Cmax 61139.150 ng/mL
Rat 10 mg/kg p.o. AUC0-t 1474.816 ng·h/mL
Rat 5 mg/kg i.v. AUC0-t 30464.355 ng·h/mL
Rat 10 mg/kg p.o. AUC0-∞ 1498.461 ng·h/mL
Rat 5 mg/kg i.v. AUC0-∞ 30509.903 ng·h/mL
Rat 10 mg/kg p.o. MRT0-t 2.961 h
Rat 5 mg/kg i.v. MRT0-t 0.645 h
Rat 10 mg/kg p.o. MRT0-∞ 3.263 h
Rat 5 mg/kg i.v. MRT0-∞ 0.689 h
Rat 10 mg/kg p.o. F 2.421 %
Rat 5 mg/kg i.v. Vss 113.508 mL/kg
Rat 5 mg/kg i.v. Vd 941.525 mL/kg
Rat 5 mg/kg i.v. CL 164.535 mL/h/kg
体内研究
(In Vivo)

Ferroptosis-IN-22 (Compound 4k) (5-15 mg/kg，腹腔注射，在注射 ConA 前 2 次给药) 可缓解由刀豆蛋白 A (ConA) (HY-P2149) 引起的铁死亡引起的急性肝损伤抑制[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ConA induced acute liver injury model established in C57BL/6J mice[1]
Dosage: 5 and 15 mg/kg
Administration: Intraperitoneal injection (i.p.), 24 hours and 0.5 hours before ConA injection
Result: Decreased serum ALT and AST levels and improved liver tissue injury.
Significantly reduced the mRNA levels of TNF-α and IL-6, two major inflammatory cytokines in the liver.
Effectively reduced the levels of4-HNE and MDA, two lipid peroxidation products, in liver tissues.
Showed no effect on the morphology and the 4-HNE level of other vital organs including kidney, spleen, heart and lung.
Reduced the mRNA expression of ferroptosis marker Ptgs2.
分子量

393.48

Formula

C27H23NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Ferroptosis-IN-22 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ferroptosis-IN-22FerroptosisFerritinophagyNCOA4 (Nuclear Receptor Coactivator 4)Pseudonatural Product (PNP)Benzofuro[2,3-b]pyridineRhodium-catalyzed C-H activationIron homeostasisLipid peroxidationAcute liver injury (ConA-induced)Inhibitorinhibitorinhibit

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