histone acetyltransferase

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.

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.

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

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.

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).

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

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).

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

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.

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.

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].

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).

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.

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

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.

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).

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

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

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.

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

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.

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

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.

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

SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor.

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.

NiCur blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC 50 value of 0.35 μΜ. NiCur can be used to perform mechanistic studies without affecting target proteins expression [1].

A-485 is a potent and selective catalytic p300/CBP inhibitor(IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively).

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

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

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

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

CBP/p300-IN-10, a potent inhibitor targeting histone acetyltransferase enzymes EP300 and CREBBP, exhibits IC50 values of 26 nM and 39 nM, respectively. This compound shows potential for anticancer research applications.

Lys-CoA TFA, a selective p300 histone acetyltransferase (HAT) inhibitor (IC 50 =50-500 nM), exhibits a specificity that exceeds 100-fold over PCAF (IC 50 =200 μM). This compound effectively suppresses transcriptional activation dependent on p300 HAT activity [1] [2].

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

Delphinidin chloride, a natural plant pigment found in berries and red wine, is a precursor of certain anthocyanins. Delphinidin chloride induces the release of nitric oxide from the vascular endothelium, resulting in vascular relaxation. At the dose of 1-40 μM, epithelial growth factor receptor signaling and estrogen receptor α expression were inhibited, which was associated with apoptosis and autophagy. Delphinidin chloride regulates JAK/STAT3 and MAPKinase signaling. Delphinidin also inhibited the histone acetyltransferase activity of p300/CBP (IC50 was about 30 μM).

P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).

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

JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.

BF1 is an inhibitor of HAT (histone acetyltransferase) active both in vitro and in vivo.

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.