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.

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.

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.

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.

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

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

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.

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

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).

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

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.

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

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

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.

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

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

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

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.

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

CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.

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

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

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.

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.