Catalog Number: 5775
Chemical Name: rel-2-[4-[6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-4H-pyrrolo[2,3-d]pyrimidin-4-one
Biological Activity
Potent TNKS2 and TNKS1 inhibitor (IC50 values are 1 and 3 nM, respectively). Exhibits >100-fold selectivity for TNKS1/2 over PARP-1, PARP-2 and PARP-6. Inhibits Wnt signaling in DLD-1 cells (IC50 = 5 nM). Exhibits moderate oral bioavailability.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
    Johannes et al.
    ACS Med.Chem.Lett., 2015;13:254
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