GSK 2837808A |
Catalog No.GC13464 |
GSK 2837808A est un inhibiteur puissant et sélectif de la lactate déshydrogénase A (LDHA) avec des IC50 de 2,6 et 43 nM pour hLDHA et hLDHB, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1445879-21-9
Sample solution is provided at 25 µL, 10mM.
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.
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