PKM2 activator 3 

PKM2 activator 3 is a potent PKM2 activator with an AC₅₀ value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer^[1].
^{(AC₅₀: the concentration which gives 50% activation of enzyme.)}

PKM2^[1]

PKM2 activator 3 (compound 66) has good Caco-2 permeability, a low efflux ratio (0.84) and high microsomal stability (t1/2 = 277.2 min in human liver microsomes and 117.5 min in mouse liver microsomes)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

372.77

C₁₅H₁₁ClF₂N₂O₃S

1346113-84-5

FC1=C(Cl)C=C(NS(=O)(C(C=C2CC3)=C(F)C=C2NC3=O)=O)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Walsh MJ, et al. 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7.  [Content Brief]