1. Metabolic Enzyme/Protease
    JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
  2. Phosphatase
    STAT
    Apoptosis
  3. SC-43

SC-43 

Cat. No.: HY-136657
Handling Instructions

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

For research use only. We do not sell to patients.

SC-43 Chemical Structure

SC-43 Chemical Structure

CAS No. : 1400989-25-4

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Description

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects[1][2].

IC50 & Target[1][2]

SHP-1

 

p-STAT3

 

In Vitro

SC-43 (0-10 μM; 24-72 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment reveals the anti-proliferative effects in cholangiocarcinoma (CCA) cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively[1].
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines[1].
SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level[1].
SC-43 activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. SC-43 augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HuCCT-1, KKU-100, and CGCCA cells
Concentration: 0 μM, 0.25 μM, 0.5 μM, 0.75 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Revealed the anti-proliferative effects in CCA cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively.

Cell Cycle Analysis[1]

Cell Line: HuCCT-1, KKU-100, and CGCCA cells
Concentration: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: Showed increased sub-G1 cells and G2-M arrest.

Western Blot Analysis[1]

Cell Line: HuCCT-1, KKU-100, and CGCCA cells
Concentration: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: Demonstrated significant increase in cleaved caspase-3 and PARP level.
In Vivo

SC-43 (10-30 mg/kg; oral gavage; daily; for 23 days; male NCr athymic nude mice) treatment exhibits xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells[1]
Dosage: 10 mg/kg or 30 mg/kg
Administration: Oral gavage; daily; for 23 days
Result: Exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
Clinical Trial
Molecular Weight

431.80

Formula

C₂₁H₁₃ClF₃N₃O₂

CAS No.

1400989-25-4

SMILES

O=C(NC1=CC=CC(OC2=CC=C(C#N)C=C2)=C1)NC3=CC=C(Cl)C(C(F)(F)F)=C3

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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.

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Keywords:

SC-43SC43SC 43PhosphataseSTATApoptosisSHP-1PTPN6antiproliferativep-STAT3anti-fibroticanticancerorallycaspase-3PARPInhibitorinhibitorinhibit

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