1. Apoptosis
  2. Apoptosis Ferroptosis
  3. Ferroptosis/apoptosis inducer-4

Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu2+/Cu+ redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca2+ release, mitochondrial Ca2+ overload, and the formation of a ROS−Ca2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer.

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Ferroptosis/apoptosis inducer-4

Ferroptosis/apoptosis inducer-4 Chemical Structure

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Description

Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu2+/Cu+ redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca2+ release, mitochondrial Ca2+ overload, and the formation of a ROS−Ca2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer[1].

In Vitro

Ferroptosis/apoptosis inducer-4 (Cu2) (incubated for 24 h) potently inhibits the viability of HeLa, MCF-7, SK-OV-3, A549 and HCT-116 tumor cells, with IC50s ranging from 0.39 μM to 1.44 μM, and exhibits low cytotoxicity against normal LX-2 cells[1].
Ferroptosis/apoptosis inducer-4 (0.4-0.8 μM) induces caspase-dependent apoptosis in HeLa cells by altering the expression of pro-apoptotic and anti-apoptotic proteins, and activating caspase-3 and caspase-9 in a dose-dependent manner[1].
Ferroptosis/apoptosis inducer-4 (0.4-0.8 μM) inhibits the migration and invasion of HeLa cells in a dose-dependent manner, and this effect is associated with the downregulated expression of MACC1[1].

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

Parmacokinetics
Species Dose Route AUC0-24 T1/2 Tmax Cmax
Mice[1] 5 mg/kg i.v. 25.6 mg·h/L 38.9 h 0.5 h 25.7 mg/L
In Vivo

Cu2+ (5 mg/kg; i.v.; every other day) exhibits superior in vivo antitumor efficacy against cervical cancer xenografts, with a 64.7% tumor growth inhibition rate, and demonstrates minimal systemic toxicity compared to cisplatin[1].
Cu2+ (5 mg/kg; i.v.) effectively inhibits HeLa cell lung metastasis in nude mice, as evidenced by reduced lung metastatic burden and lower lung wet weight[1].

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

Animal Model: Nude mice with Cervical cancer[1]
Dosage: 5 mg/kg
Administration: i.v.; every other day
Result: Achieved a tumor growth inhibition rate (TGI) of 64.7%.
Showed continued body weight increase during treatment.
Showed no statistically significant differences in major organ (heart, liver, spleen, lung, kidney) weights compared to control mice.
Showed no obvious pathological damage observed in H&E-stained organ sections.
Molecular Weight

481.65

Formula

C14H15Br2CuFN4

SMILES

CC(C1=[N]2NC3=[N]([Cu+2]2([Br-])([N]4=C1C=CC=C4)[Br-])C=CC(F)=C3)C

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  • 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.

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Product Name:
Ferroptosis/apoptosis inducer-4
Cat. No.:
HY-183549
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