ZX703
ZX703 is a GPX4 PROTAC degrader with a DC50 of 0.135 μM. ZX703 degrades GPX4 via the ubiquitin-proteasome and autophagy-lysosome pathways. ZX703 induces the accumulation of ROS, thereby triggering Ferroptosis. ZX703 can be used in studies related to fibrosarcoma and prostate cancer.
(Pink: GPX4 ligand (HY-100003); Blue: VHL ligand (HY-125845); Black: linker (HY-Y0148)).
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- 화학식: C54H67ClN8O9S
- 분자량:1039.68
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
제품 설명
IC50 & Target
[1]|
GPX4 0.135 μM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-1080 | IC50 |
0.435 μM
Compound: 5i; ZX703
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Antiproliferative activity against human HT-1080 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK-8 assay
Antiproliferative activity against human HT-1080 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK-8 assay
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[PMID: 38505849] |
In Vitro
ZX703 (24 h) inhibits HT1080 cell growth with an IC50 of 0.435 μM, showing greater potency than analogs with altered linker length or VHL ligand structure[1].
ZX703 inhibits DU145 cell growth with an IC50 of 0.369 μM[1].
ZX703 (0-5 μM; 0-24 h) potently degrades GPX4 in HT1080 cells in vitro in a dose- and time-dependent manner, with a DC50 of 0.135 μM and sustained degradation for at least 24 h[1].
ZX703 (0.25-1.0 μM; 12 h) induces dose-dependent ROS accumulation in HT1080 cells, leading to ferroptosis that can be rescued by the ferroptosis inhibitor Fer-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT1080 cells
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Concentration:0-5 μM (dose-dependent assay); 0.2 μM (time-course assay)
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Incubation Time:0-24 h (time-course assay)
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Result:Induced dose-dependent GPX4 degradation with a DC50 of 0.135 μM and a maximum degradation (Dmax) of 86%.
In the time-course assay, ~50% of GPX4 was degraded after 6 h, over 80% was degraded after 12 h, and degradation activity persisted for at least 24 h.
Chemical Information
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분자량 1039.68
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화학식 C54H67ClN8O9S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCOC2=CC=C(C(C3=CC=C(Cl)C=C3)N4CCN(C(C5=NOC(C)=C5[N+]([O-])=O)=O)CC4)C=C2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZX703 Related Classifications
HY-157788 Related Classifications
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