MG 149

MG149 (Tip60 HAT inhibitor) 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 inhibits KAT8 and blocks PINK1 kinase activity. MG149 inhibits the phosphorylation of Parkin and ubiquitin, thereby suppressing the initiation of PINK1-dependent mitophagy. MG 149 can reverse chronic restraint stress (CRS) induced hypertension and related molecular changes. MG 149 commonly used in research on diseases such as hypertension and Parkinson's disease^[1][2][3]. IC50 & Target:IC50: 74/47 μM (Tip60/MOF)^[1] In Vitro:MG 149 (Tip60 HAT inhibitor), at 200 μM, inhibited about 90% of Tip60 activity but had no inhibitory impact on p300 and PCAF. MG 149 was essentially competitive with Ac-CoA and noncompetitive with the histone substrate. HAT inhibition studies with MG 149 demonstrated that both compounds inhibited the HAT activity of the nuclear extracts of different regions significantly (p < 0.05)^[1].
MG 149 (100 μM, 3 h) inhibits the activation of the PINK1/Parkin pathway in POE SH-SY5Y cells^[2]. In Vivo:MG 149 (1.6 mg/kg, i.p., once daily, for 14 days) can reverse chronic restraint stress (CRS) induced hypertension in male C57BL/6J mice^[3].