1. PROTAC JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. PROTACs STAT MDM-2/p53
  3. 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: Ligands for Target Protein for PROTAC ligand (HY-163526); Blue: Ligands for E3 Ligase ligand (HY-10984); Black: linker (HY-130447)).

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S3D5

S3D5 Chemical Structure

CAS No. : 3033746-21-0

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Description

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[1]. (Pink: Ligands for Target Protein for PROTAC ligand (HY-163526); Blue: Ligands for E3 Ligase ligand (HY-10984); Black: linker (HY-130447)).

IC50 & Target

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.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM
Incubation Time: 24 h
Result: Induced STAT3 degradation in HepG2 cells.

Cell Proliferation Assay[1]

Cell Line: HepG2 cells
Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 14 days
Result: Led to a significant reduction in both the number and size of HepG2 cells.

Cell Invasion Assay[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Significantly inhibited the invasive ability of HepG2 cells.

Cell Migration Assay [1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Significantly inhibited the migration ability of HepG2 cells.
Molecular Weight

956.89

Formula

C41H45F5N6O13S

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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S3D5
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HY-179243
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