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Submit ReviewGSK 2837808A
说明： Potent and selective LDHA inhibitor
化学名： 3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid
纯度： ≥98% (HPLC)
生物活性 for GSK 2837808A
GSK 2837808A is a potent and selective lactate dehydrogenase A and B (LDHA and LDHB) inhibitor (IC50 values are 2.6 and 43 nM for LDHA and LDHB respectively). Inhibits lactate production in selected cancer cell lines. Reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells. Inhibits proliferation and induces apoptosis in Snu398 cells. Inhibits transcription of histone 2B (H2B) gene in HCT116 and NCM460 cells. Cell permeable.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline.
化合物库 for GSK 2837808A
GSK 2837808A is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK 2837808A
| 分子量 | 649.62 |
| 公式 | C31H25F2N5O7S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1445879-21-9 |
| PubChem ID | 71533725 |
| InChI Key | RZBCPMYJIARMGV-UHFFFAOYSA-N |
| Smiles | O=S(C2=C(NC3=CC(OC5=CC(F)=CC(F)=C5)=CC(C(O)=O)=C3)C1=CC=C(C6=CN=C(OC)N=C6OC)C=C1N=C2)(NC4CC4)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GSK 2837808A
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 64.96 | 100 |
制备储备液 for GSK 2837808A
以下数据基于产品分子量 649.62。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.54 mL | 7.7 mL | 15.39 mL |
| 5 mM | 0.31 mL | 1.54 mL | 3.08 mL |
| 10 mM | 0.15 mL | 0.77 mL | 1.54 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
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产品说明书 for GSK 2837808A
参考文献 for GSK 2837808A
参考文献是支持产品生物活性的出版物。
Billiard et al (2013) Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 1 19 PMID: 24280423
Xie et al (2014) Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells. Cell.Metab. 19 795 PMID: 24726384
Brighenti et al (2017) The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis. Biochem.Biophys.Res.Commun. 485 742 PMID: 28257841
If you know of a relevant reference for GSK 2837808A, please let us know.
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关键词: GSK 2837808A, GSK 2837808A supplier, GSK2837808A, potent, selective, lactate, dehydrogenase, A, LDHA, inhibitors, inhibits, H2B, transcription, Lactate, Dehydrogenase, 5189, Tocris Bioscience
17 篇 GSK 2837808A 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK 2837808A 的部分引用包括：
Nidhi et al (2021) The distinct roles of calcium in rapid control of neuronal glycolysis and the tricarboxylic acid cycle. Elife 10 PMID: 33555254
Catherine A et al (2021) Fructose reprogrammes glutamine-dependent oxidative metabolism to support LPS-induced inflammation. Nat Commun 12 1209 PMID: 33619282
David A et al (2022) A high-throughput multiparameter screen for accelerated development and optimization of soluble genetically encoded fluorescent biosensors. Nat Commun 13 2919 PMID: 35614105
Jacqueline D et al (2022) Tumor-Derived Lactic Acid Modulates Activation and Metabolic Status of Draining Lymph Node Stroma. Cancer Immunol Res 10 482-497 PMID: 35362044
Cascone et al (2018) Increased Tumor Glycolysis Characterizes Immune Resistance to Adoptive T Cell Therapy. Cell Metab 27 977 PMID: 29628419
David E et al (2020) Lactate production is a prioritized feature of adipocyte metabolism. J Biol Chem 295 83-98 PMID: 33518012
Georg et al (2020) Metabolic reprogramming of osteoclasts represents a therapeutic target during the treatment of osteoporosis. Sci Rep 10 21020 PMID: 33273570
David E et al (2020) Lactate production is a prioritized feature of adipocyte metabolism. J Biol Chem 295 83-98 PMID: 31690627
Merk et al (2016) Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery. Cell 165 1698 PMID: 27238019
Sylvie et al (2023) Mitochondrial pyruvate metabolism regulates the activation of quiescent adult neural stem cells. Sci Adv 9 eadd5220 PMID: 36857455
Randall S et al (2023) Lactate exposure shapes the metabolic and transcriptomic profile of CD8+ T cells. Front Immunol 14 1101433 PMID: 36923405
Lin et al (2017) Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop. Oncotarget 8 110426 PMID: 29299159
Diaz-Garcia et al (2017) Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake. Cell Metab 26 361 PMID: 28768175
Thongon et al (2018) Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA. Cancer Metab 6 1 PMID: 29541451
Hanse et al (2017) Cytosolic malate dehydrogenase activity helps support glycolysis in actively proliferating cells and cancer. Oncogene 36 3915 PMID: 28263970
Brighenti et al (2017) The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis. Biochem.Biophys.Res.Commun. 485 742 PMID: 28257841
Massey (2017) Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. Sci Rep 7 40778 PMID: 28106079
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Mouse oocytes lactate uptake.
By
Anonymous on 11/13/2023
分析类型： In Vitro
种属： Mouse
细胞系/组织： Oocytes
GSK 2837808A inhibitor titrations were performed at pH 6 with oocytes preincubated for 45 min in a different uptake buffer (75 mM NaCl,2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Mes, pH 6)containing the required concentration of GSK 2837808A prior tomeasuring the uptake of L-[14C]lactate (0.5 mM).
该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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