Cookie Policy: This site uses cookies to improve your experience. You can find out more about our use of cookies in our Privacy Policy. By continuing to browse this site you agree to our use of cookies.
AdipoGen Life Sciences
GSK2837808A
55
CHF
CHF 55.00
In stock
AG-CR1-3685-M0011 mgCHF 55.00
AG-CR1-3685-M0055 mgCHF 220.00
| Product Details | |
|---|---|
| Synonyms | 3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid |
| Product Type | Chemical |
| Properties | |
| Formula |
C31H25F2N5O7S |
| MW | 649.6 |
| CAS | 1445879-21-9 |
| Purity Chemicals | ≥98% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (30mg/ml) or DMF (30mg/ml). |
| InChi Key | RZBCPMYJIARMGV-UHFFFAOYSA-N |
| Smiles | FC1=CC(F)=CC(OC2=CC(C(O)=O)=CC(NC3=C(C=NC4=C3C=CC(C5=C(N=C(N=C5)OC)OC)=C4)S(NC6CC6)(=O)=O)=C2)=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and selective cell permeable inhibitor of lactate dehydrogenase A (LDHA) (IC50 values are 2.6 and 43 nM for LDHA and LDHB, respectively). Decreases glycolysis.
- Useful agent for immunometabolism research.
- Exhibits antitumoral activity. 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.
- Lactate dehydrogenase A (LDHA) is an important enzyme involved in fermentative glycolysis, important in tumor initiation and metabolism. Cancer cells rely on increased glycolysis resulting in increased lactate production in addition to aerobic respiration in the mitochondria, even under normal oxygen concentrations (a process known as the Warburg effect). This renders LDHA a promising molecular target for the treatment of various cancers.
Product References
- Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells: J. Billiard, et al.; Cancer Metab. 1, 19 (2013)
- Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor initiating cells: H. Xie, et al.; Cell Metab. 19, 795 (2014)
- A guide to immunometabolism for immunologists: L.A. O'Neill, et al.; Nat. Rev. Immunol. 16, 553 (2016)
- The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis: E. Brighenti, et al.; BBRC 485, 742 (2017)
Related Products
