505487 Sigma-AldrichPKM2 Activator IV, TEPP-46 - Calbiochem
PKM2 Activator IV, TEPP-46, CAS 1221186-53-3, is a cell-permeable, allosteric PKM2 activator (AC50 = 92 nM) that stabilizes PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2.
More>> PKM2 Activator IV, TEPP-46, CAS 1221186-53-3, is a cell-permeable, allosteric PKM2 activator (AC50 = 92 nM) that stabilizes PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2. Less<<Synonymes: 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46
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Tableau de caractéristiques principal
CAS # | Empirical Formula |
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1221186-53-3 | C₁₇H₁₆N₄O₂S₂ |
Prix & Disponibilité
Référence | Disponibilité | Conditionnement | Qté | Prix | Quantité | |
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5054870001 |
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Flacon en verre | 5 mg |
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Description | |
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Overview | A cell-permeable thienopyrrolopyridazinone that exhibits good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) by stabilizing PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2 (2 activator/4 FBP/tetramer) in a similar manner as PKM2 Activator III (Cat. No. 504537). Reprorted to retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro and impair H1299 tumorigenesis in mice (50 mg/kg/12 h p.o.) in vivo with no apparent toxicity. |
Catalogue Number | 505487 |
Brand Family | Calbiochem® |
Synonyms | 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46 |
References | |
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References | Anastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839. Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387. |
Product Information | |
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CAS number | 1221186-53-3 |
Form | White solid |
Hill Formula | C₁₇H₁₆N₄O₂S₂ |
Chemical formula | C₁₇H₁₆N₄O₂S₂ |
Reversible | Y |
Structure formula Image | |
Quality Level | MQ100 |
Biological Information | |
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Primary Target | PKM2 |
Purity | ≥98% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
Global Trade Item Number | |
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Référence | GTIN |
5054870001 | 04055977243383 |