Pyruvate Kinase Activator

Code: 550601-25MG D2-231

General description

A cell-permeable (Papp x 106 = 9.38 and 7.91 cm/s, respectively, for 'A-B' and 'B-A' in Caco-2 permeability assay) and biologically ...


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€245.40 EACH
€301.84 inc. VAT

General description

A cell-permeable (Papp x 106 = 9.38 and 7.91 cm/s, respectively, for 'A-B' and 'B-A' in Caco-2 permeability assay) and biologically stable (t1/2 = 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 (Km = 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; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.

A cell-permeable and biologically stable (t1/2 = 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 (Km = 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; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.

Legal Information

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

Other Notes

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

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Standard Handling (A)

assay≥98% (HPLC)
colorwhite
formpowder
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
SMILES stringFC1=CC2=C(CCC(N2)=O)C=C1S(NC3=CC=C(F)C(Cl)=C3)(=O)=O
solubilityDMSO: 100 mg/mL, clear, colorless
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number1346113-84-5
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