gcn5

Butyrolactone 3 (MB-3) is a histone acetyltransferase Gcn5 inhibitor with a weak affinity for CBP.Butyrolactone 3 has antimicrobial activity and has been used in cancer, metabolic and neurological disorders.

BRD-IN-3 is a highly potent PCAF bromodomain (BRD) inhibitor (IC50: 7 nM). It also exhibits activity against GCN5 and FALZ.

GSK4028 is the enantiomeric negative control of GSK4027, a PCAF GCN5 bromodomain chemical probe, with a pIC50 of 4.9 in a TR-FRET assay.

GSK 4027 is a PCAF GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

PU139 is a novel inhibitor of histone acetyltransferase (HAT).

GSK699 is a potent, cell penetrant PCAF GCN5 PROTAC.

High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID:27966810

YF-2 hydrochloride is a potent histone acetyltransferase activator that exhibits high selectivity and can pass through the blood-brain barrier. It specifically acetylates H3 in the hippocampus, with EC50 values of 2.75 μM, 29.04 μM, and 49.31 μM for CBP, PCAF, and GCN5, respectively. Notably, it does not affect HDAC activity. Moreover, YF-2 hydrochloride demonstrates promising anti-cancer and anti-Alzheimer's disease properties.

YF-2 is blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, CBP, PCAF, and GCN5 with EC50s of 2.75 μM, 29.04 μM and 49.31 μM , respectively

F2276-0104 is a PCAF GCN5 BRD inhibitor

F2276-0106 is a PCAF GCN5 BRD inhibitor

F2276-0008 is a PCAF GCN5 BRD inhibitor.

F2276-0099 is a PCAF GCN5 BRD inhibitor

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

CPTH6, a thiazole derivative, selectively inhibits the lysine acetyltransferase activity of Gcn5 and pCAF without affecting p300 or CBP. It effectively blocks the acetylation of H3/H4 histones and α-tubulin in various leukemia cell lines, leading to reduced cell viability by arresting the cell cycle in the G0/G1 phase and inducing apoptosis. Additionally, CPTH6 disrupts autophagy across several tumor cell lines, primarily by interfering with ATG7-mediated autophagosomal membrane elongation.

SGF29-IN-1 (Compound Cpd_DC60) serves as a selective inhibitor targeting the Tudor domain of the Spt-Ada-Gcn5 acetyltransferase (SAGA)-associated factor 29 (SGF29). It has demonstrated effectiveness in treating leukemia [1].