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Description

A cell-permeable benzylidenbarbituric acid derivative that acts as a potent, selective inhibitor of lysine acetyltransferase p300/CBP paralogues (IC50 = 2.9 µ,M and 1.1 µ,M for recombinant p300 and CBP, respectively). The inhibition appears to be reversible and is non-competitive with respect to both acetyl-CoA and a histone H3 peptide. It binds to both the free enzyme and the enzyme-substrate complex with uneven affinities. Does not affect the activity of general control non-derepressible 5 (GCN5) and p300/CBP-associated factor (PCAF). Shown to reduce the acetylation of lysine H4K5 and H3K9 in U937 cells (~100 µ,M) and induce a cell cycle arrest at the G0/G1 phase with an increase in the percentage of hypodiploid nuclei (~ 100 µ,M).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable benzylidenbarbituric acid derivative that acts as a potent, selective inhibitor of lysine acetyltransferase p300/CBP paralogues (IC50 = 2.9 µ,M and 1.1 µ,M for recombinant p300 and CBP, respectively). The inhibition appears to be reversible and is non-competitive with respect to both acetyl-CoA and a histone H3 peptide. It binds to both the free enzyme and the enzyme-substrate complex with uneven affinities. Does not affect the activity of general control non-derepressible 5 (GCN5) and p300/CBP-associated factor (PCAF). Shown to reduce the acetylation of lysine H4K5 and H3K9 in U937 cells (~100 µ,M) and induce a cell cycle arrest at the G0/G1 phase with an increase in the percentage of hypodiploid nuclei (~ 100 µ,M).