S3D5
S3D5 is a highly efficient and selective PROTAC degrader targeting STAT3 (KD = 4.35 μM). S3D5 induces degradation of STAT3 in HepG2 cells without significant effects on other STAT proteins. S3D5 exhibits good anti-hepatocellular carcinoma cell proliferation activity, which can be explained by activating the p53 pathway. S3D5 degradation of the STAT3 protein is mediated by the ubiquitin–proteasome system (UPS). S3D5 can be used for the study of hepatocellular carcinoma.
(Pink: STAT3 ligand (HY-163526); Blue: Cereblon ligand (HY-10984); Black: linker (HY-130447)).
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- CAS No.: 3033746-21-0
- Formule: C41H45F5N6O13S
- Masse moléculaire:956.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
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STAT3 4.35 μM (Kd) |
In Vitro
S3D5 (4-20 μM, 96 h) shows optimal activity in HepG2 cells, with an IC50 value of 8.53 μM[1].
S3D5 (0.1-2 μM, 24-48 h) can induce STAT3 degradation in HepG2 cells (DC50 = 110 nM), and have little effect at any concentration on STAT1, STAT2, STAT4, STAT5, and STAT6 proteins[1].
S3D5 (2.5-20 μM, 96 h) inhibits the growth of HepG2 cells in a dose-dependent manner and inhibits the proliferation of 293T cells at 5 μM[1].
S3D5 (1-20 μM, 14 days) leads to a significant reduction in both the number and size of HepG2 cell colonies compared to the control[1].
S3D5 (5μM, 24-72 h) can inhibit the proliferation, migration and invasion of HepG2 cells[1].
S3D5 (0.1-2 μM, 48 h) dose-dependently upregulates p53 and p21 protein levels, while downregulates STAT3 protein levels in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.1 μM, 0.2 μM, 0.5 μM
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Incubation Time:24 h
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Result:Induced STAT3 degradation in HepG2 cells.
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Cell Line:HepG2 cells
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Concentration:1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:14 days
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Result:Led to a significant reduction in both the number and size of HepG2 cells.
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Cell Line:HepG2 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Significantly inhibited the invasive ability of HepG2 cells.
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Cell Line:HepG2 cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Significantly inhibited the migration ability of HepG2 cells.
Chemical Information
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CAS No. 3033746-21-0
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Masse moléculaire 956.89
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Formule C41H45F5N6O13S
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SMILES
CN(S(=O)(C1=C(C(F)=C(C(F)=C1F)F)F)=O)CC(NC2=CC=C(C=C2)C(NCCOCCOCCOCCOCCOCCNC3=C4C(C(N(C5C(NC(CC5)=O)=O)C4=O)=O)=CC=C3)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S3D5 Related Classifications
HY-179243 Related Classifications
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