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AdipoGen Life Sciences
TEPP46 [ML-265]
50
CHF
CHF 50.00
In stock
AG-CR1-3687-M0011 mgCHF 50.00
AG-CR1-3687-M0055 mgCHF 120.00
AG-CR1-3687-M02525 mgCHF 420.00
| Product Details | |
|---|---|
| Synonyms | TEPP-46; ML265; NCGC00186528; CID-44246499 |
| Product Type | Chemical |
| Properties | |
| Formula |
C17H16N4O2S2 |
| MW | 372.5 |
| CAS | 1221186-53-3 |
| Purity Chemicals | ≥95% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (10mg/ml). Insoluble in water. |
| Identity | Determined by 1H-NMR |
| InChi Key | ZWKJWVSEDISQIS-UHFFFAOYSA-N |
| Smiles | CS(C1=CC(N2C)=C(C3=C2C(N(N=C3)CC4=CC(N)=CC=C4)=O)S1)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| 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 pyruvate kinase M2 (PKM2) activator with little or no activity versus PKM1, PKL and PKR.
- Useful agent for immunometabolism research.
- Anticancer (reducing tumor sizes in mice) and anti-inflammatory agent.
- Shown to bind the enzyme PKM2 to promote formation of stable, enzymatically-active tetramers, thereby promoting the last rate-limiting step of glycolysis, converting PEP to pyruvate. In addition, it prevents PKM2 translocation to the nucleus resulting in reduced glycolysis and HIF-1α activation, causing diminished Warburg effect and IL-1β production.
Product References
- J.K. Jiang et al. Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase: J.K. Jiang, et al.; Bioorg. Med. Chem. Lett. 20, 3387 (2010)
- ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model: M.J. Walsh, et al.; Probe Rep. NIH Mol. Libr. Prog. (2012)
- Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis: D. Anastasiou, et al.; Nat. Chem. Biol. 8, 839 (2012)
- Pyruvate Kinase M2 regulates HIF-1α activity and IL-1β induction and is a critical determinant of the Warburg effect in LPS-activated macrophages: E.M. Palsson-McDermott, et al.; Cell Metab. 21, 65 (2015)
- A guide to immunometabolism for immunologists: L.A. O'Neill, et al.; Nat. Rev. Immunol. 16, 553 (2016)
- Pyruvate Kinase M2: A Potential Target for Regulating Inflammation: J.C. Alves-Filho & E.M. Palsson-McDermott; Front. Immunol. 7, 145 (2016) (Review)
- Similarities and Distinctions of Cancer and Immune Metabolism in Inflammation and Tumors: G. Andrejeva & J.C. Rathmell; Cell Metab. 26, 49 (2017)
- Targeting metabolism as a novel therapeutic approach to autoimmunity, inflammation and transplantation: I.A. Bettencourt & J.D. Powell; J. Immunol. 198, 999 (2017)
- Caloric Restriction Mimetic 2-Deoxyglucose Alleviated Inflammatory Lung Injury via Suppressing Nuclear Pyruvate Kinase M2-Signal Transducer and Activator of Transcription 3 Pathway: K. Hu, et al.; Front. Immunol. 9, 426 (2018)
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