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  5. R&D Systems™ TEPP 46

R&D Systems™ TEPP 46
SDP

Catalog No. RD10195096 Shop All Novus Products
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RD10195096 10 mg
RD10195076 50 mg
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Catalog No. RD10195096 Supplier R&D Systems™ Supplier No. 7809/10

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Description

A Tocris product, part of R&D Systems. 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. It also inhibits experimental autoimmune encephalomyelitis (EAE) in vivo. Orally bioavailable.

Specifications

Chemical Name or Material 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
Quantity 10 mg
Product Line Tocris
Target PKM2
Molecular Formula C17H16N4O2S2
Purity 0.98
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