Pyruvate Kinase Activator-Calbiochem

C₁₅H₁₁ClF₂N₂O₃S

372.77

A cell-permeable (P_app x 10⁶ = 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t_1/2 = 277.2 and 117.5 min., respectively, using human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP (phosphoenolpyruvate), but not the acceptor ADP, substrate affinity toward PK (pyruvate kinase) isoform PKM2 (K_m = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC₅₀ = 90 nM using rhPKM2; AC_max = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.
A cell-permeable and biologically stable (t_1/2 = 277.2 and 117.5 min., respectively, in human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP, but not the acceptor ADP, substrate affinity toward pyruvate kinase isoform PKM2 (K_m = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC₅₀ = 90 nM using rhPKM2; AC_max = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Walsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett.21, 6322.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥98% (HPLC)

powder

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 100 mg/mL, clear, colorless

ambient

2-8℃

FC1=CC2=C(CCC(N2)=O)C=C1S(NC3=CC=C(F)C(Cl)=C3)(=O)=O

25 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3