2592638-14-5

CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 μM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity[1].

Myst3: >100 μM (IC₅₀); p300-HAT: 1.4 μM (IC₅₀); CBP-HAT: 2.2 μM (IC₅₀); PCAF: >100 μM (IC₅₀)

[1] Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407. DOI:10.1016/j.ejmech.2022.114407