chemical

7809/10

7809/10

10 mg (also 50 mg)

121 USD

7809/10

TEPP 46

10 mg (also 50 mg)

Potent and selective pyruvate kinase M2 (PKM2) allosteric activator

PKM2

Small Molecules

98%

372.47

?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

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 . It also inhibits experimental autoimmune encephalomyelitis (EAE) in vivo . Orally bioavailable.

Potent and selective pyruvate kinase M2 (PKM2) allosteric activator

Potent and selective pyruvate kinase M2 (PKM2) allosteric activator

6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2 ,3 :4,5]pyrrolo[2,3-d]pyridazin-5-one

C17H16N4O2S2

C17H16N4O2S2

1221186-53-3

121 USD

Potent and selective pyruvate kinase M2 (PKM2) allosteric activator

CTHBP, Cytosolic thyroid hormone-binding protein, MGC3932, OIP3, OIP-3, OIP3EC 2.7.1.40, Opa-interacting protein 3, p58, PK, muscle type, PK2, PK3, PK3PKM, Pyruvate kinase 2/3, pyruvate kinase isozymes M1/M2, Pyruvate kinase muscle isozyme, pyruvate kinase, muscle, TCB, THBP1, THBP1p58, Thyroid hormone-binding protein 1, thyroid hormone-binding protein, cytosolic, Tumor M2-PK

Store at -20░C