PKM2 activator 3

Names

[ CAS No. ]:
1346113-84-5

[ Name ]:
PKM2 activator 3

Biological Activity

[Description]:

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.)

[Related Catalog]:

Research Areas >> Cancer

[Target]

PKM2[1]


[In Vivo]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H11ClF2N2O3S

[ Molecular Weight ]:
372.77

Related Compounds