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PROTAC HK2 Degrader-1

CAS No. :

MCE 站：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。

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 ubiquitinproteasome 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  |  Kinase Inhibitor Library  |  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  |  2-Deoxy-D-glucose-¹³C  |  2-Deoxy-D-glucose  |  3-Bromopyruvic acid  |  Lonidamine  |  2-Deoxy-D-glucose-¹³C-1  |  Metrizamide  |  2-Deoxy-D-glucose-d

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