STAT3-IN-53
STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 3113051-34-3
- Formula: C33H33F3N8O3S
- Molecular Weight:678.73
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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STAT3 6.16 μM (Kd) |
STAT3-IN-53 directly binds to recombinant full-length wild-type STAT3 protein with a Kd of 6.16 μM[1].
STAT3-IN-53 (concentration gradient) potently inhibits the IL-6/JAK/STAT3 signaling pathway in HEK-BLUE-IL6 cells with an IC50 of 0.89 ± 0.07 μM[1].
STAT3-IN-53 (concentration gradient; 96 h) potently inhibits the proliferation of HCT116, HT29, SW480, MC38, and CT26 colorectal cancer cell lines, with the highest activity in HCT116 cells (IC50 = 0.45 ± 0.05 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, HT29, SW480, MC38, CT26 colorectal cancer cell lines
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Concentration:concentration gradient (for IC50 determination)
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Incubation Time:96 h
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Result:Exhibited potent antiproliferative activity across all tested colorectal cancer cell lines, with IC50 values of 0.45 ± 0.05 μM (HCT116), 1.80 ± 0.10 μM (HT29), 9.34 ± 0.79 μM (SW480), 2.33 ± 0.48 μM (MC38), and 5.14 ± 0.84 μM (CT26).
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Cell Line:HCT116 cells
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Concentration:0.5, 2.5 μM
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Incubation Time:24 h
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Result:Dose-dependently suppressed STAT3 phosphorylation at the Y705 residue without altering total STAT3 protein levels.
Did not inhibit phosphorylation of STAT6 or SRC.
Dose-dependently downregulated cyclin-D1 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, SPF grade, 18-20 g, subcutaneous implantation of MC38 colon adenocarcinoma tumor fragments)[1]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:i.p.; once daily; 12 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 53.6% at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 59.8% at 20 mg/kg.
Suppressed STAT3 Y705 phosphorylation in tumor tissues at 20 mg/kg.
Downregulated Cyclin-D1 and c-Myc protein expression in tumor tissues at 20 mg/kg.
Caused no treatment-related adverse events or body weight loss exceeding 10% during the 12-day dosing period.
Chemical Information
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CAS No. 3113051-34-3
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Molecular Weight 678.73
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Formula C33H33F3N8O3S
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SMILES
O=C(OCC)C1=NC=CC(C2=NN=C(NC3=C(N4CCN(CC)CC4)C=C5N(C6CC6)C(C7=CC=C(OC(F)(F)F)C=C7)=NC5=C3)S2)=C1
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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)
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