Biological Activity
SC-43 is a derivative of sorafenib, an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6), which reduces liver fibrosis. SC-43 can reduce p-STAT3 and induce apoptosis, and has antitumor activity.
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.
Its treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines.
Its (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level.
Its activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. Its augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.
Cell Cycle Analysis
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Cell Line:
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HuCCT-1, KKU-100, and CGCCA cells
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Concentration:
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0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:
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24 hours
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Result:
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Showed increased sub-G1 cells and G2-M arrest.
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Western Blot Analysis
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Cell Line:
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HuCCT-1, KKU-100, and CGCCA cells
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Concentration:
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0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:
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24 hours
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Result:
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Demonstrated significant increase in cleaved caspase-3 and PARP level.
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