产品
编 号：F762864
分子式：C32H28Cl2N6O5
分子量：647.51
分子式：C32H28Cl2N6O5
分子量：647.51
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 3033812-84-6
产品详情
生物活性：
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research.
体内研究：
PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 需要提及造模动物是什么~）抑制4T1肿瘤模型的肿瘤生长。PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 能诱导GSDME依赖性的热化反应，实现肿瘤免疫反应，有效抑制乳腺肿瘤的生长。PROTAC HK2 Degrader-1 (Cisplatin (HY-17394) 10mg/kg, i.v., C-02 50mg/kg, i.p., 25 days, six-weekold female BALB/c mice) 可以使顺铂增敏，同时减少顺铂的结肠副作用，具有潜在的临床价值。Animal Model:xenograft models , into six-weekold female BALB/c mice
Dosage:50 mg/kg
Administration:Intraperitoneal injection, bid, for nine times.
Result:Reduced proliferation and damaged nuclei in mouse models.Increased the levels of Cytokines IL-1β, IFN-γ, and TNF-α significantly and decreased the level of TGF-β and IL-10. Elevated levels of cleaved-Casp-3 and GSDME-N in tumor tissues of mouse.
Animal Model:breast tumor model in mice by injecting 4T1 cells subcutaneously into six-weekold female BALB/c mice
Dosage:Cisplatin (HY-17394) 10mg/kg, 50mg/kg
Administration:Cisplatin (HY-17394) (10mg/kg, i.v.), 50mg/kg, i.p., 25 days
Result:Inhibited tumor growth and tumor volume.Decreased HK2 protein level, while co- treated with Cisplatin (HY-17394).Could alleviate Cisplatin (HY-17394) aggravated colon damage.
体外研究：
PROTAC HK2 Degrader-1 抑制 786-O，4T1，PANC-1，HGC-27，MCF-1 细胞增殖的 IC50 分别为34.07 μM，5.08 μM，31.53 μM，6.11 μM，21.65 μM。PROTAC HK2 Degrader-1 对 HK2 的 DC50 为2.56 μM (4T1) 和 0.79 μM (MDA-MB-231)。PROTAC HK2 Degrader-1 (0.01-200 μM, 36 h) 选择性地抑制乳腺癌细胞增殖，并通过泛素介导的蛋白酶体途径，以时间和浓度依赖的方式刺激HK2蛋白的降解。PROTAC HK2 Degrader-1 (10 μM for 4T1, 0.5 μM for MDA-MB-231, 24 h) 通过泛素-蛋白酶体系统形成一个三元复合体降解HK2蛋白。这一句可作为机制，放到产品总描述中。PROTAC HK2 Degrader-1 (20 μM, 36 h) 降解HK2导致线粒体损伤后释放细胞色素C激活caspase-3，裂解GSDME引发热昏迷从而细胞释放危险信号，如ATP、HMGB1、CRT等，最后导致诱发细胞免疫死亡。PROTAC HK2 Degrader-1 (20 μM, 36 h) 能诱导 PD-L1 蛋白从细胞膜内化到细胞质，并减少 PD-L1 蛋白的总量。
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research.
体内研究：
PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 需要提及造模动物是什么~）抑制4T1肿瘤模型的肿瘤生长。PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 能诱导GSDME依赖性的热化反应，实现肿瘤免疫反应，有效抑制乳腺肿瘤的生长。PROTAC HK2 Degrader-1 (Cisplatin (HY-17394) 10mg/kg, i.v., C-02 50mg/kg, i.p., 25 days, six-weekold female BALB/c mice) 可以使顺铂增敏，同时减少顺铂的结肠副作用，具有潜在的临床价值。Animal Model:xenograft models , into six-weekold female BALB/c mice
Dosage:50 mg/kg
Administration:Intraperitoneal injection, bid, for nine times.
Result:Reduced proliferation and damaged nuclei in mouse models.Increased the levels of Cytokines IL-1β, IFN-γ, and TNF-α significantly and decreased the level of TGF-β and IL-10. Elevated levels of cleaved-Casp-3 and GSDME-N in tumor tissues of mouse.
Animal Model:breast tumor model in mice by injecting 4T1 cells subcutaneously into six-weekold female BALB/c mice
Dosage:Cisplatin (HY-17394) 10mg/kg, 50mg/kg
Administration:Cisplatin (HY-17394) (10mg/kg, i.v.), 50mg/kg, i.p., 25 days
Result:Inhibited tumor growth and tumor volume.Decreased HK2 protein level, while co- treated with Cisplatin (HY-17394).Could alleviate Cisplatin (HY-17394) aggravated colon damage.
体外研究：
PROTAC HK2 Degrader-1 抑制 786-O，4T1，PANC-1，HGC-27，MCF-1 细胞增殖的 IC50 分别为34.07 μM，5.08 μM，31.53 μM，6.11 μM，21.65 μM。PROTAC HK2 Degrader-1 对 HK2 的 DC50 为2.56 μM (4T1) 和 0.79 μM (MDA-MB-231)。PROTAC HK2 Degrader-1 (0.01-200 μM, 36 h) 选择性地抑制乳腺癌细胞增殖，并通过泛素介导的蛋白酶体途径，以时间和浓度依赖的方式刺激HK2蛋白的降解。PROTAC HK2 Degrader-1 (10 μM for 4T1, 0.5 μM for MDA-MB-231, 24 h) 通过泛素-蛋白酶体系统形成一个三元复合体降解HK2蛋白。这一句可作为机制，放到产品总描述中。PROTAC HK2 Degrader-1 (20 μM, 36 h) 降解HK2导致线粒体损伤后释放细胞色素C激活caspase-3，裂解GSDME引发热昏迷从而细胞释放危险信号，如ATP、HMGB1、CRT等，最后导致诱发细胞免疫死亡。PROTAC HK2 Degrader-1 (20 μM, 36 h) 能诱导 PD-L1 蛋白从细胞膜内化到细胞质，并减少 PD-L1 蛋白的总量。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备