Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

Phosphate acetyltransferase, a transferase enzyme utilized in biochemical research, catalyzes the reversible acetylation of CoA from acetyl-P, yielding acetyl-CoA and inorganic phosphate. This process is integral to acetate assimilation/dissimilation reactions [1].

Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.

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.

Polygalacic acid (Virgaureagenin G)(PA) significantly improves cholinergic system reactivity, as indicated by decreased acetylcholinesterase (AChE) activity, increases choline acetyltransferase (ChAT) activity, and elevates levels of acetylcholine (ACh) in the hippocampus and frontal cortex, PA also significantly ameliorates neuroinflammation and oxidative stress in mice; suggest that PA might exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation. Polygalacic acid shows significant postingestive effects on Spodoptera littoralis larvae.

Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.

MC4033 is a selective lysine acetyltransferase 8 (KAT8) inhibitor (IC50: 12.1 μM) with anticancer effects, induces apoptosis, and can be used for the study of non-small cell lung cancer.

JG-2016, as a small molecule histone acetyltransferase 1 (HAT1) inhibitor, inhibits the growth of human cancer cell lines, inhibits enzyme activity in cellulose, and interferes with tumor growth.

CID-4785700 is a potent pan-GTPase inhibitor that inhibits Rab7 and inhibits the fungal histone acetyltransferase Rtt109 that binds to Asf1 and Vps75, and can be used in the study of lupus.

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

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

Diethylnorspermine HCl (N1,N11-Diethylnorspermine tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively stabilizes SSAT enzyme activity.

NEO2734 (EP31670) is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).

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.

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).

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.

MeIQx (MeIQx) is a food-derived carcinogen that has been found in high temperature-cooked fish and meats.1It is activated by hydroxylation and subsequent O-acetylationviathe cytochrome P450 (CYP) isoform CYP1A2 and N-acetyltransferase 2, respectively, in UV5 cells expressing the human enzymes to a metabolite that reacts with DNA to form adducts.2MeIQx (200 and 400 ppm in the diet) induces tumor formation in rats.3

Naa50-IN-1 (Compound 4a) is a potent inhibitor of N-α-Acetyltransferase 50 (Naa50), demonstrating an IC50 of 7 mM, with potential applications in cancer research [1].

Monosodium N-acetylglutamate is the sodium salt of N-acetylglutamate, biosynthesized from glutamate and acetylornithine by ornithine acetyltransferase, and from glutamic acid and acetyl-CoA by the enzyme N-acetylglutamate synthase.

Isepamicin (Sch 21420) is a potent aminoglycoside antibacterial compound with enhanced efficacy against strains harboring type I 6'-acetyltransferase. Its antibacterial spectrum encompasses Enterobacteriaceae and staphylococci, while exhibiting resistance against anaerobes, Neisseriaceae, and streptococci. Moreover, Isepamicin displays a robust concentration-dependent bactericidal effect, a prolonged post-antibiotic effect lasting several hours, and is capable of inducing adaptive resistance.

α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC 50 of 9 μM. α-NETA is a potent ALDH1A1 ( IC 50 =0.04 μM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC 50 =84 μM) and acetylcholinesterase (AChE; IC 50 =300 μM). α-NETA has anti-cancer activity [1] [2].

ZSET-845 is an enhancer of cognitive which enhances choline acetyltransferase activity in the hippocampus in the rat.

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.

PU141 is a novel inhibitor of histone acetyltransferase (HAT).

MeAIB is an N-acetyltransferase inhibitor that inhibits SNAT2-related signaling pathways. MeAIB is a specific substrate for amino acid transport system a (ATA1). Amino acid transport system a (ATA1) regulates the uptake of short chain neutral amino acids by Na+ flow.

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.

Acetyl phosphate lithium potassium (Lithium potassium acetyl phosphate) is a compound involved in taurine and hypotaurine metabolism as well as pyruvate metabolism. Acetyl phosphate lithium potassiu is generated from sulfoacetaldehyde, converted to acetyl-CoA and acetate via phosphate acetyltransferase and acetate kinase respectively. Acetyl phosphate lithium potassiu is also an intermediate in pyruvate metabolism.

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

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

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

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

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.

CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.

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

4-Acetamidophenyl acetate is an impurity of Acetaminophen. Acetaminophen is a selective COX-2 inhibitor (IC50: 25.8 μM) and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

TH1834 is a selective inhibitor of the Tip60 (KAT5) histone acetyltransferase (HAT). It effectively induces apoptosis and promotes DNA damage in breast cancer cells. Notably, TH1834 does not influence the activity of the MOF histone acetyltransferase, which is structurally related. Overall, TH1834 exhibits potent anticancer activity.

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.

N-acetylglucosamine-1-P uridyltransferase (AGX1) (GlcNAc1pUT) is a bifunctional enzyme that couples with GlcNAc-1-P and UTP to catalyze the synthesis of UDP-GlcNAc through an uridyltransfer reaction. It exhibits acetyltransferase and uridyltransferase activities, and its presence is exclusive to prokaryotes [1].

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].

MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP. This compound enhances the expression of TRAIL apoptotic genes while concurrently suppressing DNA damage response pathways. Its structure comprises a CBP/p300 binding domain, a p53Y220C targeting moiety, and a connecting linker [1].

Histone H3 (1-21) is a truncated form of the Histone H3 protein consisting of amino acids 1 to 21. It serves as a common substrate for methyltransferase assays targeting Histone 3 at lysine 4 and lysine 9, as well as for acetyltransferase assays targeting Histone 3 at lysine 9 and lysine 14.

Selective p300 histone acetyltransferase (HAT) inhibitor (IC50 = 50-500 nM). Exhibits approximately 100-fold selectivity for p300 over PCAF (IC50 = 200 μM). Inhibits p300-dependent transcription. Active in vivo. Lau et al (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol.Cell. 5 589 PMID:10882143 |Liu et al (2008) The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451 846 PMID:18273021 |Burns et al (2005) Iso-coenzyme A. J.Biol.Chem. 280 16550 PMID:15708855 |Cebrat et al (2003) Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg.Med.Chem. 11 3307 PMID:12837541

CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.

CAY10685 is a cell-active analog of the lysine acetyltransferase inhibitor CPTH2 that contains an alkyne moiety for use in click chemistry reactions. Its ability to inhibit N-acetyltransferase 10 activity has been used to modulate chromatin organization in order to study changes in nuclear architecture associated with cancer and certain laminopathies.

1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.

CTX-0124143 is a histone acetyltransferase inhibitor with an IC50 value of 1.0 μM for KAT6A.CTX-0124143 can be used to study cellular senescence.

Amifampridine is mainly used to treat many rare muscle diseases. In the United States, aminopyridine is being studied for the treatment of Lambert-Eaton myasmus syndrome (LEMS). Amifampridine is also used to treat many congenital myasthenia syndromes, par

ANAT Inhibitor-1 serves as an inhibitor of human aspartate N-acetyltransferase (ANAT), targeting Canavan disease.

NAT2-IN-1 (APA) is a selective inhibitor of the drug metabolism enzyme N-acetyltransferase 2 (NAT2), capable of targeting and eliminating cells with slow NAT2 activity [1].