MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149, at 200 μM, inhibites about 90% of Tip60 activity but has no inhibitory impact on p300 and PCAF. MG 149 is essentially competitive with Ac-CoA and noncompetitive with the histone substrate. MG149 inhibits acetyltransferase activity of nuclear extract from tissue samples from different brain regions in mice. MG149 inhibits the p53 and the NF-κB pathways.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mM|
Basic nuclear processes affected by histone acetyltransferases and histone deacetylase inhibitors.
Legartová S, et al. Epigenomics. 2013 Aug;5(4):379-96. PMID: 23895652.
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WM-8014, also known as MOZ-IN-3, is a highly potent inhibitor of MOZ with an IC50 of 55 nM.
YF2 is a selective HAT (histone acetyltransferase) activator, with EC50 values of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF and GCN5, respectively.
Remodelin hydrobromide is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
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