histone acetyltransferase

A-485 is a potent and selective catalytic p300 CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

NEO2734 (EP31670) is an orally active, selective inhibitor of p300/CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

NU 9056 is an effective and selective inhibitor of KAT5 histone acetyltransferase with an IC50 of 2 µM. NU 9056 blocks DNA damage response and inhibits protein acetylation in prostate cancer cell lines.

Remodelin is an effective and specific inhibitor of the acetyl-transferase protein NAT10.

CPI-637 is a selective and cell-active benzodiazepinone CBP EP300 bromodomain inhibitor.

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione)  as a bona fide is a potent p300/CBP inhibitor

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

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.

CTPB is a potent p300 histone acetyltransferase (HAT) activator that can be used in the preparation of hair growth promoters and/or hair loss treatments.

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP p300 bromodomains.

WM-1119 is a highly potent, selective KAT6A/B inhibitor

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

Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.

MG 149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF(IC50= 47 uM).

MOZ-IN-3 (Compound 6j), a potent KAT6A (MOZ) acetyltransferase inhibitor with an IC50 of 30 nM, exhibits antitumor activity against multiple myeloid leukemia cell lines, including HL-60, U937, SKNO-1, and K562. This compound also demonstrates favorable metabolic stability and pharmacokinetics [1].

MC4171 is a selective KAT8 inhibitor with antiproliferative activity and can be used to study cancer.

KAT modulator-1 (Compound 3), an epigenetics research tool, selectively interacts with the full-length p300 protein but not its catalytic domain [1].