GlpBio

GSK 2837808A

目录号: GC13464纯度: >99.00%
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。
GSK 2837808A
Cas No.: 1445879-21-9
规格价格库存数量操作
2mg¥665.00现货
1
5mg¥1,260.00现货
1
10mg¥2,030.00现货
1
25mg¥4,060.00现货
1
50mg¥6,510.00现货
1
100mg¥10,360.00现货
1
10mM (in 1mL DMSO)¥2,101.00现货
1
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产品描述 Description

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]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

NPC (nasopharynx) cells

Preparation Method

Reaction Conditions

10 µM;24-72h

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]:

Animal models

Female C57BL/6 mice

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.

Dosage form

6 mg/kg/day; p.o ;4weeks

Applications

GSK2837808A decreased tumor weight, decreased tumor volume, and increased tumor cell apoptosis.

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.
[2]. 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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1445879-21-9
化学名
3-((3-(N-cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid
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 g/mol
溶解性
DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol