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TEPP-46
- ML265
- Soluble in DMSO
- MF: C17H16N4O2S2
- MW: 372.46
Description
Potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR. Continuous dosing of mice with TEPP-46 decreased the development of human cancer cell xenografts, suggesting that increased pyruvate kinase activity can impair tumorigenesis.TEPP-46 can mimic the enzymatic properties of PKM1 in PKM2-expressing cells, alter cell metabolism, and induces changes in the kinetic properties of PKM2 that are identical to those induced by the endogenous PKM2 activator FBP.
More Information
| Parent CAS No. | 1221186-53-3 |
|---|---|
| Chemical Name | 6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-Thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one |
| SMILES | C1C=CC(N)=CC=1CN1C(=O)C2N(C)C3C=C(S(C)=O)SC=3C=2C=N1 |
| MFCD | N.A. |
| 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 |
| CID | 44246499 |
| Short Description | PKM2 activator |
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. Bioorg. Med. Chem. Lett. 2010, 20, 3387–3393.
- D. Anastasiou et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat. Chem. Biol. 2012, 8, 839-847.
- M.J. Walsh et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. Probe Reports from the NIH Molecular Libraries Program.
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