PARP Inhibitor XI, DR2313 from Calbiochem

2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidine-4-one

White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A brain-permeable and water soluble pyrimidinone compound that acts as a potent and NAD⁺-competitive inhibitor of PARP (IC₅₀ = 200 nM and 240 nM for rhPARP1 and rmPARP2, respectively) with little activity against the dehydrogenase activity of GAPDH, ADH, LDH, or the ADP-ribosylase activity of bacterial diphtheria toxin even at concentrations as high as 10 µM. Shown to inhibit H₂O₂-induced PAR formation and neuronal cell death in primary rat cerebral cortex culture in vitro (EC₅₀ = 270 nM) and exhibit neuroprotective effects in both permanent and transient focal ischemia models in rat in in vivo. Purity: ≥98% by HPLC. Soluble in H₂O. CAS 284028-90-6, M.W. 182.2.