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產(chǎn)品名稱

TEPP 46 - ML 265

產(chǎn)品貨號(hào)

Axon 2240 CAS [1221186-53-3] MF C17H16N4O2S2MW 372.46 Purity: 99% Soluble in DMSO 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. KEYWORDS:? TEPP 46 | supplier | PKM2 activator ?| ML 265 | TEPP46 | ML265 | TEPP-46 | ML-265 | CAS [1221186-53-3] | Pyyruvate | PKM2 | Activator | Enzymes | ?Glycolysis | Warburg | tumorigenesis | cancer | glucose metabolism

產(chǎn)品價(jià)格

現(xiàn)貨詢價(jià)，電話：010-67529703

產(chǎn)品規(guī)格

產(chǎn)品品牌

axonmedchem

產(chǎn)品概述

產(chǎn)品詳情

TEPP 46 - ML 265

Based on 12 reference(s) in Google Scholar 9 10 12

Axon 2240

CAS [1221186-53-3]

MF C17H16N4O2S2
MW 372.46

Purity: 99%
Soluble in DMSO

TEPP 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.

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.?

Certificate of Analysis
Material Safety Data Sheet

Cell Signaling & Oncology Diabetes & Metabolism Immunology PKM2 EC 2.7.1.40

Potent activator of recombinant PKM2 with little or no activity versus PKM1, PKL and PKR.

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

Parent CAS No.

[1221186-53-3]

產(chǎn)品資料

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