| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | SC-43 | ||||||||||||
| CAS | 1400989-25-4 | ||||||||||||
| Formula | C21H13ClF3N3O2 | ||||||||||||
| Molar Mass | 431.80 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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