TEPP46 [ML-265]
| Code | Size | Price |
|---|
| AG-CR1-3687-M001 | 1 mg | £45.00 |
Quantity:
| AG-CR1-3687-M005 | 5 mg | £100.00 |
Quantity:
| AG-CR1-3687-M025 | 25 mg | £310.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Target Species: Universal
Shipping:
AMBIENT
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
TEPP-46; ML265; NCGC00186528; CID-44246499
Appearance:
White to off-white solid.
CAS:
1221186-53-3
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C17H16N4O2S2/c1-20-13-7-14(25(2)23)24-16(13)12-8-19-21(17(22)15(12)20)9-10-4-3-5-11(18)6-10/h3-8H,9,18H2,1-2H3
InChiKey:
ZWKJWVSEDISQIS-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1221186-53-3. Formula: C17H16N4O2S2. MW: 372.5. . 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-1alpha activation, causing diminished Warburg effect and IL-1beta production.
MDL:
MFCD23160747
Molecular Formula:
C17H16N4O2S2
Molecular Weight:
372.5
Package Type:
Vial
Product 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-1alpha activation, causing diminished Warburg effect and IL-1beta production.
Purity:
>95%
SMILES:
CS(C1=CC(N2C)=C(C3=C2C(N(N=C3)CC4=CC(N)=CC=C4)=O)S1)=O
Solubility Chemicals:
Soluble in DMSO (10mg/ml). Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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-1alpha activity and IL-1beta 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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