PROTAC HK2 Degrader-1 | MedChemExpress (MCE)

PROTAC HK2 Degrader-1 产品活性：PROTAC HK2 Degrader-1 是靶向 Hexokinase 2 (HK2) 的 PROTAC。PROTAC HK2 Degrader-1 由 Hexokinase 2 (HK2) 抑制剂 Lonidamine (HY-B0486)，CRBN 配体 Thalidomide (HY-14658) 组成。PROTAC HK2 Degrader-1通过泛素-蛋白酶体系统形成一个三元复合体降解 Hexokinase 2 (HK2) 蛋白诱导线粒体损伤，引发细胞焦亡 (pyroptosis)。PROTAC HK2 Degrader-1 能有效抑制乳腺肿瘤的生长，并减少 Cisplatin (HY-17394) 的结肠副作用。可用于乳腺癌的研究。 产品来源： https://www.medchemexpress.cn/protac-hk2-degrader-1.html 研究领域：Metabolic Enzyme/Protease 作用靶点：Hexokinase In Vitro: PROTAC HK2 Degrader-1 inhibits the proliferation of 786-O, 4T1, PANC-1, HGC-27, and MCF-1 with IC50s of 34.07 μM, 5.08 μM, 31.53 μM, 6.11 μM, and 21.65 μM, respectively. PROTAC HK2 Degrader-1 degrades HK2 with DC50 values of was 2.56 μM (4T1) and 0.79 μM (MDA-MB-231), respectively. PROTAC HK2 Degrader-1 (0.01-200 μM, 36 h) selectively suppresses breast cancer cell proliferation and stimulates HK2 protein degradation via the ubiquitin mediated proteasome pathway in a time and concentration dependent manner. PROTAC HK2 Degrader-1 (10 μM for 4T1, 0.5 μM for MDA-MB-231, 24 h) degraded HK2 protein via the ubiquitin−proteasome system by forming a ternary complex. PROTAC HK2 Degrader-1 (20 μM, 36 h) mediates degradation of HK2 that causing mitochondrial damage, releasing cytochrome C to activate caspase-3, then PROTAC HK2 Degrader-1 cleaves GSDME to trigger thermal coma and promotes cellular release of danger signals, such as ATP, HMGB1, CRT, etc., thus inducing cellular immune death. PROTAC HK2 Degrader-1 (20 μM, 36 h) can induce PD-L1 protein to internalize from the cell membrane to the cytoplasm and reduce the total amount of PD-L1 protein. In Vivo: PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, into six-weekold female BALB/c mice) inhibits tumor growth in 4T1 tumor models. PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) can induce GSDME-dependent pyroptosis to realize tumor immune response and effectively inhibit breast tumor growth. PROTAC HK2 Degrader-1 (Cisplatin (HY-17394) 10mg/kg, i.v., C-02 50mg/kg, i.p., 25 days, into six-weekold female BALB/c mice) can sensitize Cisplatin (HY-17394) while reducing the colon side effects of Cisplatin (HY-17394), which has potential clinical value. 相关产品：Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Glycolysis Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Glucose Metabolism Compound Library | Metabolic Enzyme Compound Library | Bioactive Compound Library Max | 2-Deoxy-D-glucose | 3-Bromopyruvic acid | Lonidamine | Metrizamide | Hexokinase 2 inhibitor 1 | Hexokinase II VDAC binding domain peptide 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。

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