PROTAC HIF-1α degrader-2
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer.
(Pink: HIF-1α ligand (HY-179434); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3095636-64-6
- Formula: C50H65N7O9S
- Molecular Weight:940.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIF-1α 22.4 μM (DC50) |
VHL |
PROTAC HIF-1α degrader-2 (Compound Z12) shows the strongest anti-proliferative activity against HeLa cells (IC50 = 10.10 μM)[1].
PROTAC HIF-1α degrader-2 (0-80 μM, 24 h) dose-dependently degrades HIF-1α protein in HeLa cells (DC50 = 22.40 μM), and high concentrations (> 40 μM) exhibit a "hook effect"[1].
PROTAC HIF-1α degrader-2 (20 μM, 0-36 h) degrades HIF-1α in HeLa cells in a time-dependent manner, with a degradation rate of 59.7% after 36 hours of incubation, and after removing the compound, the degradation effect could be maintained for 24 hours[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 48 h) induces acute cytotoxicity in HeLa cells, dose-dependently reducing live cells (green fluorescence) and increasing dead cells (red fluorescence)[1].
PROTAC HIF-1α degrader-2 (0-10 μM, 15 days) dose-dependently inhibits HeLa cell colony formation[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 0-24 h) inhibits the migration ability of HeLa cells[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 24-48 h) induces apoptosis, morphological changes in HeLa cells, and increases the apoptosis rate of HeLa cells[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 24 h) dose-dependently reduces the protein levels of p-MEK (44.6%-89.1%) and p-AKT (39.0%-63.0%) in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 60 μM, 80 μM
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Incubation Time:24 h
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Result:Dose-dependently degraded HIF-1α protein, with a DC50 of 22.40 μM and a maximum degradation rate (D%) of 73% (at 40 μM). A "hook effect" was observed at high concentrations (> 40 μM).
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Cell Line:HeLa cells
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Concentration:0 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:0 h, 6 h, 24 h
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Result:Dose-dependently degraded HIF-1α protein, with a DC50 of 22.40 μM and a maximum degradation rate (D%) of 73% (at 40 μM). A "hook effect" was observed at high concentrations (> 40 μM).
Chemical Information
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CAS No. 3095636-64-6
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Molecular Weight 940.16
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Formula C50H65N7O9S
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SMILES
COC(C1=CC(NC(COC2=CC=C(C=C2)N3CCN(CC3)CCCCCCCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)=O)=O)=C(C=C1)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC HIF-1α degrader-2 Related Classifications
HY-179424 Related Classifications
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