CBP/p300-IN-19

CBP/p300-IN-19 is a potent 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 shows antitumor activity[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

p300:1.4 μM (IC50)

PCAF:2.2 μM (IC50)

CBP:>100 μM (IC50)

Myst3:>100 μM (IC50)

CBP/p300-IN-19 (compound 29) shows antiproliferative activity with EC50s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively[1]. CBP/p300-IN-19 (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27[1]. Western Blot Analysis[1] Cell Line: Kasumi-1 leukemia cells Concentration: 0, 5, 10 µM Incubation Time: 12 h Result: Dose-dependently inhibited the acetylation of H3K18, H3K9 and K27.

[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.