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SC-43

CAT: 0013-GTR19157803-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19157803-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.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. In vivo assay revealed that SC-43 exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
CAS Number
1400989-25-4
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 250 mg/mL (578.97 mM)
Smiles
FC (F) (F) c1cc (NC (=O) Nc2cccc (Oc3ccc (cc3) C#N) c2) ccc1Cl
Molecular Formula
C21H13ClF3N3O2?
Molecular Weight
431.8
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.