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505487 PKM2 Activator IV, TEPP-46 - Calbiochem

505487
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Overview

Key Spec Table

CAS #Empirical Formula
1221186-53-3C₁₇H₁₆N₄O₂S₂

Products

Catalogue NumberPackaging Qty/Pack
5054870001 Glass bottle 5 mg
Description
OverviewA 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 Number505487
Brand Family Calbiochem®
Synonyms6-((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
ReferencesAnastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.
Product Information
CAS number1221186-53-3
FormWhite solid
Hill FormulaC₁₇H₁₆N₄O₂S₂
Chemical formulaC₁₇H₁₆N₄O₂S₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationPKM2 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.
Biological Information
Primary TargetPKM2
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
5054870001 04055977243383