DC Chemicals Limited
China
Product Name: SC-43
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1400989-25-4

1400989-25-4 structure

1400989-25-4 structure

Name: SC-43
Chemical Name: SC-43
CAS Number: 1400989-25-4
Molecular Formula: C₂₁H₁₃ClF₃N₃O₂
Molecular Weight: 431.80
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2021-01-08 12:29:06
Modify Date: 2024-01-01 21:35:01
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].

Name	SC-43
Synonyms	MFCD31380911

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].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> STAT Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase Signaling Pathways >> JAK/STAT Signaling >> STAT
Target	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]. 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]. 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.
References	[1]. Ming-Hung Hu, et al. Targeting SHP-1-STAT3 signaling: A promising therapeutic approach for the treatment of cholangiocarcinoma. Oncotarget. 2017 May 10;8(39):65077-65089. [2]. Tung-Hung Su, et al. Src-homology protein tyrosine phosphatase-1 agonist, SC-43, reduces liver fibrosis. Sci Rep. 2017 May 11;7(1):1728.

Molecular Formula	C₂₁H₁₃ClF₃N₃O₂
Molecular Weight	431.80