TEPP 46

Product Description

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.

Licensing Information

Sold under licence from the National Institute of Health.

Solubility

Preparing Stock Solutions for TEPP 46

The following data is based on the product molecular weight 372.47

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.68 mL	13.42 mL	26.85 mL
5 mM	0.54 mL	2.68 mL	5.37 mL
10 mM	0.27 mL	1.34 mL	2.68 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Angiari Pharmacological activation of pyruvate kinase M2 inhibits CD4+ T Cell pathogenicity and suppresses autoimmunity. Cell Metab. 2020 PMID: 31761564
• Taylor Dietary fructose improves intestinal cell survival and nutrient absorption. Nature 2021 PMID: 34408323
• Anastasiou Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat.Chem.Biol. 2012 PMID: 22922757