GSK 2837808A | Tocris Bioscience 5189/10 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

GSK 2837808A

catalog :

5189/10

quantity :

10 mg

price :

368 USD

more info or order :

Tocris Bioscience product webpage

citations: 8

Reference
Cascone T, McKenzie J, Mbofung R, Punt S, Wang Z, Xu C, et al. Increased Tumor Glycolysis Characterizes Immune Resistance to Adoptive T Cell Therapy. Cell Metab. 2018;27:977-987.e4 pubmed publisher
Thongon N, Zucal C, D Agostino V, Tebaldi T, Ravera S, Zamporlini F, et al. Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA. Cancer Metab. 2018;6:1 pubmed publisher
Lin S, Sun L, Lyu X, Ai X, Du D, Su N, et al. 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. 2017;8:110426-110443 pubmed publisher
Diaz Garcia C, Mongeon R, Lahmann C, Koveal D, Zucker H, Yellen G. Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake. Cell Metab. 2017;26:361-374.e4 pubmed publisher
Hanse E, Ruan C, Kachman M, Wang D, Lowman X, Kelekar A. Cytosolic malate dehydrogenase activity helps support glycolysis in actively proliferating cells and cancer. Oncogene. 2017;36:3915-3924 pubmed publisher
Brighenti E, Carnicelli D, Brigotti M, Fiume L. The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis. Biochem Biophys Res Commun. 2017;485:742-745 pubmed publisher
Massey A. Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. Sci Rep. 2017;7:40778 pubmed publisher
Merk A, Bartesaghi A, Banerjee S, Falconieri V, Rao P, Davis M, et al. Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery. Cell. 2016;165:1698-1707 pubmed publisher

product information

brand :

Tocris

master code :

5189

SKU :

5189/10

rank :

0.061

product name :

GSK 2837808A

description :

Potent and selective LDHA inhibitor

target :

Lactate Dehydrogenase A/LDHA Inhibitors

category :

Small Molecules

sizes available :

10 mg

url print :

?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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.

extended description :

Potent and selective LDHA inhibitor

chemical name text :

3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid

formula :

C 31 H 25 F 2 N 5 O 7 S

formula text :

C31H25F2N5O7S

cas num :

1445879-21-9

USD :

368 USD

product details :

Potent and selective LDHA inhibitor

storage :

Store the unopened product at -20 to -70 °C. Use a manual defrost freezer and avoid repeated freeze-thaw cycles. Do not use past expiration date.

more info or order :

Tocris Bioscience product webpage