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SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $96 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $537 | In Stock | |
50 mg | $768 | In Stock | |
100 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $226 | In Stock |
Description | SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects. |
In vitro | SC-43, a sorafenib derivative.SC-43-induced apoptosis in cholangiocarcinoma (CCA) via a novel mechanism.?Three CCA cell lines (HuCCT-1, KKU-100 and CGCCA) were treated with SC-43 to determine their sensitivity to SC-43-induced cell death and apoptosis.?SC-43 activated SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation, which induced G2-M arrest and apoptotic cell death.?Importantly, SC-43 augmented SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.?Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 counteracted the effect of SC-43-induced SHP-1 phosphatase activation and antiproliferation ability in CCA cells[1]. |
In vivo | In vivo assay revealed that SC-43 exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation[1]. |
Molecular Weight | 431.8 |
Formula | C21H13ClF3N3O2 |
Cas No. | 1400989-25-4 |
Smiles | FC(F)(F)c1cc(NC(=O)Nc2cccc(Oc3ccc(cc3)C#N)c2)ccc1Cl |
Relative Density. | 1.46 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (231.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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