化合物SC-43 T8478

Product Introduction
Bioactivity


英文名: SC-43

描述: SC-43 是一种具有口服活性的SHP-1 (PTPN6)激动剂。它是Sorafenib 的衍生物，可抑制STAT3的磷酸化并诱导细胞凋亡，具有抗纤维化和抗癌作用。

体外活性: 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].

体内活性: 体内实验显示，SC-43显示了抑制异种移植瘤生长、降低p-STAT3以及提高SHP-1活性的效果[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (231.59 mM)


关键字: antiproliferative | Inhibitor | SHP-1 | PTPN6 | Phosphatase | SC43 | Apoptosis | caspase-3 | SC-43 | anti-fibrotic | p-STAT3 | anticancer | orally | PARP | STAT | SC 43 | inhibit

相关产品: Brazilin | Tanespimycin | Floxuridine | PF-543 hydrochloride | Asperosaponin VI | Bromelain | PI-103 | Flavokawain C | Taraxerol | Thapsigargin

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Cancer Cell Differentiation Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途