Potent and selective pyruvate kinase M2 (PKM2) allosteric activator
TEPP 46 is a potent and selective allosteric activator of pyruvate kinase M2 (PKM2) (EC50 = 92 nM); it exhibits no effect on PKM1. TEPP 46 binds at the dimer-dimer interface of the PKM2 homotetramer, blocks its translocation into the nuclues and promotes a constitutively PKM2 active state. TEPP 46 impairs H1299 lung cancer cell proliferation under hypoxic conditions but not under normoxia
in vitro
. It inhibits growth of H1299 tumor xenografts in mice. TEPP 46 can reverse fructose-derived F1P inhibition of PKM2 and prevent fructose promoted hypoxia adaptation of intestinal cells. TEPP 46 reduces activation, proliferation, and cytokine production of both T helper 17 (Th17) and Th1 cells
in vitro
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151311 |
| Réf. fabricant | 18055962 |
| Nom chimique ou matériau | 6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one |
| CAS | 1221186-53-3 |
| Quantité | 10 mg |
| Cible | PKM2 |
| Formule moléculaire | C<sub>17</sub>H<sub>16</sub>N<sub>4</sub>O<sub>2</sub>S<sub>2</sub> |
| Pureté | 0.98 |
