GSK 2837808A
目录号 : GC13464
GSK2837808A 是一种选择性的 LDHA (lactate dehydrogenase A) 的抑制剂,对hLDHA和hLDHB的IC50分别为2.6 nM和43 nM.GSK2837808A(10 µM;24-72h)通过促进有氧糖酵解、增殖、细胞周期和细胞凋亡抵抗,阻断了着丝粒蛋白N (CENP-N)过表达对鼻咽癌细胞的影响。
Cas No.:1445879-21-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
NPC (nasopharynx) cells |
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Preparation Method |
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Reaction Conditions |
10 µM;24-72h |
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Applications |
GSK2837808A blocked the effect of Centromere protein N (CENP-N) overexpression on NPC cells by promoting aerobic glycolysis, proliferation, cell cycling and apoptosis resistance. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6 mice |
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Preparation Method |
Tumors (KPC and CAF cells) were allowed to grow for 10 days. One group of mice received GSK2837808A at a dose of 6 mg/kg/every day orally while another group received vehicle control. |
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Dosage form |
6 mg/kg/day; p.o ;4weeks |
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Applications |
GSK2837808A decreased tumor weight, decreased tumor volume, and increased tumor cell apoptosis. |
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References: [1]. Qi CL, Huang ML, et,al. The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. doi: 10.1186/s13046-021-02191-3. PMID: 34893086; PMCID: PMC8662847. |
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GSK2837808A is a selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB[1].
GSK2837808A(10 µM;24-72h) blocked the effect of Centromere protein N (CENP-N) overexpression on NPC cells by promoting aerobic glycolysis, proliferation, cell cycling and apoptosis resistance[2]. GSK2837808A(0, 5, 10, 20 µM) reversed the occurrence of low ratio of ATP/AMP, high level of Adenosine Monophosphate-activated Protein Kinase (AMPK) activation, disturbed HAS2 synthesis and hyaluronic acid (HA) production by inhibiting LDHA in TMJ osteoarthritis synovial fibroblasts (TMJOA SFs)[3].
GSK2837808A(6 mg/kg/day;p.o;4weeks) treatment, KPC and CAF tumor weight and tumor volume decreased significantly, tumor lactate to lactate: pyruvate ratio decreased significantly, and apoptosis of tumor cells increased in mice[4].
References:
[1]. Billiard J, Dennison JB, et,al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. doi: 10.1186/2049-3002-1-19. PMID: 24280423; PMCID: PMC4178217.
[2]. Qi CL, Huang ML, et,al. The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. doi: 10.1186/s13046-021-02191-3. PMID: 34893086; PMCID: PMC8662847.
[3]. Li HM, Guo HL, et,al. Inhibition of glycolysis by targeting lactate dehydrogenase A facilitates hyaluronan synthase 2 synthesis in synovial fibroblasts of temporomandibular joint osteoarthritis. Bone. 2020 Dec;141:115584. doi: 10.1016/j.bone.2020.115584. Epub 2020 Aug 11. PMID: 32795674.
[4].Gupta VK, Sharma NS, et,al. Hypoxia-Driven Oncometabolite L-2HG Maintains Stemness-Differentiation Balance and Facilitates Immune Evasion in Pancreatic Cancer. Cancer Res. 2021 Aug 1;81(15):4001-4013. doi: 10.1158/0008-5472.CAN-20-2562. Epub 2021 May 14. PMID: 33990397; PMCID: PMC8338764.
GSK2837808A 是一种选择性的 LDHA (lactate dehydrogenase A) 的抑制剂,对hLDHA和hLDHB的IC50分别为2.6 nM和43 nM[1].
GSK2837808A(10 µM;24-72h)通过促进有氧糖酵解、增殖、细胞周期和细胞凋亡抵抗,阻断了着丝粒蛋白N (CENP-N)过表达对鼻咽癌细胞的影响[2]。GSK2837808A(0、5、10、20 µM)通过抑制LDHA逆转TMJ骨关节炎滑膜成纤维细胞(TMJOA SFs)中ATP/AMP比例低、腺苷单磷酸活化蛋白激酶(AMPK)激活水平高、干扰HAS2合成和透明质酸(HA)产生的现象[3]。
GSK2837808A(6 mg/kg/day; p.o;4weeks)治疗后,小鼠肿瘤重量和肿瘤体积明显减小,肿瘤乳酸与乳酸:丙酮酸比值明显降低,肿瘤细胞凋亡增加[4]。
| Cas No. | 1445879-21-9 | SDF | |
| 化学名 | 3-((3-(N-cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid | ||
| Canonical SMILES | O=S(C(C=N1)=C(NC2=CC(OC3=CC(F)=CC(F)=C3)=CC(C(O)=O)=C2)C(C1=C4)=CC=C4C5=CN=C(OC)N=C5OC)(NC6CC6)=O | ||
| 分子式 | C31H25F2N5O7S | 分子量 | 649.62 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble | 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 | 1.5394 mL | 7.6968 mL | 15.3936 mL |
| 5 mM | 0.3079 mL | 1.5394 mL | 3.0787 mL |
| 10 mM | 0.1539 mL | 0.7697 mL | 1.5394 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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