GSK620是一种具有口服活性的泛溴结构域和末端外结构域蛋白第二溴结构域的（pan-BET BD2）选择性抑制剂。
Cas No.:2088410-46-0
Sample solution is provided at 25 µL, 10mM.
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GSK620 is an orally active, pan-Bromodomain and Extra-Terminal protein Bromodomain 2 (pan-BET BD2) selective inhibitor. GSK620 is highly selective for the BET-BD2 family of proteins, with more than 200-fold selectivity over all other bromodomains[1].
In vitro, the IC₅₀ values of GSK620 in GSC23 and GSC11 cells were 38.74μM and 35.39μM, respectively. Treatment with GSK620 at 0.5-5μM for 24-48h effectively downregulated Mesenchymal (MES) gene expression in glioblastoma (GBM) models. In GSC11 and GSC23 cells, 1μM GSK620 for 24h reduced chromatin-bound BD2 and its occupancy at MES promoters; 0.5μM inhibited invasion, and 0.5-5μM suppressed colony formation[2].
In vivo, GSK620, administered orally in mice, has a plasma half-life of 1.05h and exhibits brain penetration. Oral GSK620 (30mg/kg; once daily for 8 days) significantly prolonged survival versus vehicle controls and reduced tumor-associated macrophage (TAM) infiltration by IHC in an orthotopic xenograft model[2].
References:
[1] Jonathan T Seal, et al. J Med Chem. 2020 Sep 10;63(17):9093-9126. [2] Massimo Petretich, et al. Curr Opin Chem Biol . 2020 Aug;57:184-193.
[2] Vadla R, Taylor B, Miyake Y, et al. BRD2 bromodomain-mediated regulation of cell state plasticity modulates therapy response in glioblastoma. Neuro Oncol. 2025;27(11):2828-2842.
GSK620是一种具有口服活性的泛溴结构域和末端外结构域蛋白第二溴结构域的（pan-BET BD2）选择性抑制剂。GSK620对BET蛋白的BD2结构域具有高度选择性，其对BD2的选择性相较于所有其他溴结构域高出200倍以上[1]。
体外实验中，GSK620在GSC23和GSC11细胞中的IC₅₀值分别为38.74μM和35.39μM。GSK620（0.5-5μM；24-48h）可下调胶质母细胞瘤（GBM）模型中间质型（MES）基因的表达。GSC11和GSC23细胞中，1μM GSK620处理24小时可降低染色质结合的BD2及其在MES启动子上的占位。0.5μM GSK620处理24小时抑制细胞侵袭，0.5-5μM GSK620处理24小时抑制克隆形成。
体内实验中，GSK620在小鼠中经口服给药后，血浆半衰期为1.05小时，并具有脑部渗透性。口服给予GSK620（30mg/kg；每日一次；持续8天）在原位异种移植模型中显著延长了小鼠的生存期，并通过免疫组化显示肿瘤相关巨噬细胞（TAM）浸润减少。
| Cell experiment [1]: | |
Cell lines | GSC11 and GSC23 cells |
Preparation Method | RNA-seq analysis was performed on GSC11 and GSC23 cells treated with GSK620 (0.5-5µM; 24-48h) to identify differentially expressed genes. |
Reaction Conditions | 0.5-5µM; 24-48h |
Applications | GSK620 treatment downregulated 194 genes in GSC11 and 384 genes in GSC23. Notably, CHI3L2, a key Mesenchymal marker implicated in immune cell infiltration in glioma10, was among the genes commonly downregulated in both lines. And also suppressed transcriptional programs associated with AP-1 and NF-κB signaling pathways. |
| Animal experiment [1]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Female BALB/c nude mice (4-5 weeks old) were used for intracranial tumor implantation. A total of 1-2×105 cells in a 3-5μL volume was injected stereotactically into the brain (1.0mm anterior and 2.0mm right to the bregma, and 3mm deep from the inner plate of the skull). Tumor growth was monitored using the FMT 2500 fluorescence tomography system. For drug treatment studies, mice received daily oral gavage of vehicle or GSK620 at 30mg/kg. The vehicle formulation consisted of 10% DMSO, 40% PEG, 5% Tween-80, and 45% saline. |
Dosage form | 30mg/kg; 8d; p.o. |
Applications | GSK620-treated mice lived significantly longer than vehicle-treated controls. IHC staining showed reduced infiltration of Tumor-Associated Macrophages (TAMs). |
References: | |
| Cas No. | 2088410-46-0 | SDF | |
| 分子式 | C18H19N3O3 | 分子量 | 325.36 |
| 溶解度 | DMSO : 62.5 mg/mL (192.09 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0735 mL | 15.3676 mL | 30.7352 mL |
| 5 mM | 614.7 μL | 3.0735 mL | 6.147 mL |
| 10 mM | 307.4 μL | 1.5368 mL | 3.0735 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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