2. PROTAC Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. HyT Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS)
  4. GPX4 degrader-1

GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.

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GPX4 degrader-1

GPX4 degrader-1 Chemical Structure

CAS No. : 3057531-85-5

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GPX4 degrader-1 Related Antibodies

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Description

GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model[1].

IC50 & Target[1]

GPX4

8.9 nM (DC50)

In Vitro

GPX4 degrader-1 (0.3-300 nM; 2-48 h) induces dose- and time-dependent proteasome-mediated GPX4 degradation in HT1080 fibrosarcoma cells, with a DC50 of 8.9 nM[1].
GPX4 degrader-1 (48 h) induces ferroptosis-mediated antiproliferative activity in HT1080, A549 and 4T1 cancer cells, with IC50 values of 130 nM, 6.4 μM and 700 nM, respectively[1].
GPX4 degrader-1 (0.5-2.0 μM for MDA; 24-48 h) increases lipid ROS and MDA in HT1080 fibrosarcoma cells[1].

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

GPX4 degrader-1 Related Antibodies
In Vivo

GPX4 degrader-1 (16-66 μmol/kg; i.p.; daily; 10 days) achieves potent, dose-dependent inhibition of tumor growth in a 4T1 murine breast cancer model[1].

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

Animal Model: BALB/c (female, 6 to 8 weeks old)[1]
Dosage: 16 μmol/kg; 33 μmol/kg; 66 μmol/kg
Administration: i.p.; daily; 10 days
Result: Induced dose-dependent tumor growth inhibition: 29.3% TGI at 16 μmol/kg, 54.6% TGI at 33 μmol/kg, and 80.5% TGI at 66 μmol/kg.
Demonstrated statistically significant superior antitumor activity compared to RSL3 at 66 μmol/kg (P < 0.01).
Reduced tumor weight in a dose-dependent manner.
Caused no significant changes in mouse body weight during the treatment period.
Molecular Weight

634.16

Formula

C38H36ClN3O4
CAS No.
SMILES

O=C(OC)[C@@H](C1)N(C(CCl)=O)[C@@H](C2=CC=C(C(NCCCC(C3=CC=CC=C3)C4=CC=CC=C4)=O)C=C2)C5=C1C6=CC=CC=C6N5
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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GPX4 degrader-1 Related Classifications

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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:

GPX4 degrader-13057531-85-5HyTGlutathione PeroxidaseFerroptosisReactive Oxygen Species (ROS)Hydrophobie taggingHT1080 fibrosarcoma cellsubiquitin-proteasome systemferroptosisGPX4reactive oxygen speciesmalondialdehydeA549 cancer cells4T1 cancer cellslipid peroxidationmurine mammary carcinoma modelInhibitorinhibitorinhibit

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