Histone Acetyltransferase

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.

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.

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.

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

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

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

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

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

PF-9363 (CTX-3648) is a potent and high selective KAT6A KAT6B inhibitor. PF-9363 can be used for the research of cancer.

WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

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

Procyanidin B3(B3) is a procyanidin dimer that is widely studied due to its high abundance in the human diet and antioxidant activity.

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

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.

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

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

WM-8014 (MOZ-IN-3) is an inhibitor of MOZ(IC50=55 nM), a member of histone acetyltransferases.

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

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

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.

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.

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.

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

MOZ-IN-2 is an protein MOZ inhibitor(IC50 of 125 μM).

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

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.

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.

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

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.

NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 of 15.9 μM against recombinant HAT p300 CBP-associated factor (PCAF) and exhibits anti-proliferative activity against certain cancer cells, making it useful for anti-cancer research.

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.

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

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

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

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

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.

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].

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.

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