MG149

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).IC50 value: 74/47 uM (Tip60/MOF) [1]Target: Tip60/MOFMG 149, at 200 μM, inhibited about 90% of Tip60 activity but had no inhibitory impact on p300 and PCAF. MG 149 was essentiallycompetitive 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 extractsof different regions significantly (p < 0.05).

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

Research Areas >> Cancer

[1]. Ghizzoni M, et al. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15