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Histone acetyltransferase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Acetyltransferase (40) Histone Demethylase (1) Aldehyde Dehydrogenase (ALDH) (1) Apoptosis (9) Autophagy (2) Bacterial (1) Chemerin Receptor (1) Cholinesterase (ChE) (2) Endogenous Metabolite (1) Epigenetic Reader Domain (6) Ferroptosis (1) Influenza Virus (1) Keap1-Nrf2 (1) MDM-2/p53 (1) Mitophagy (1) STAT (1)
By Research Areas:	Cancer (42) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (5)

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Targets Recommended: Histone Acetyltransferase Histone Methyltransferase Histone Demethylase HDAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100734

Histone Acetyltransferase Inhibitor II	Histone Acetyltransferase	Cancer
Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC₅₀ of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells .

HY-W013274

CPTH2	Histone Acetyltransferase Apoptosis	Cancer
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .

HY-129039

Butyrolactone 3 5 Publications Verification MB-3	Histone Acetyltransferase	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC₅₀=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC₅₀=0.5 mM). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases .

HY-W013274A

CPTH2 hydrochloride	Histone Acetyltransferase Apoptosis	Cancer
CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .

HY-147261

B026	Histone Acetyltransferase	Cancer
B026 is a selective, potent, orally active *p300/CBP histone* acetyltransferase (HAT) inhibitor with IC₅₀** values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines .

HY-131035

Lys-CoA TFA	Histone Acetyltransferase	Cancer
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC₅₀=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC₅₀=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation .

HY-13823

C646 50+ Cited Publications	Histone Acetyltransferase Autophagy Epigenetic Reader Domain Apoptosis	Cancer
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases .

HY-123604A

TH1834 dihydrochloride 1 Publications Verification	Histone Acetyltransferase Apoptosis	Cancer
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .

HY-116673

TTK21	Histone Acetyltransferase	Neurological Disease
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .

HY-123604

TH1834 1 Publications Verification	Histone Acetyltransferase Apoptosis	Cancer
TH1834 is a specific *Tip60 (KAT5) histone* acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis** and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .

HY-102060

WM-8014

2 Publications Verification

Histone Acetyltransferase Cancer

WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC₅₀ of 55 nM.
HY-102059

MOZ-IN-2

Histone Acetyltransferase Cancer

MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC₅₀ of 125 μM.
HY-138945

SYY-B085-1

Histone Acetyltransferase Cancer

SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor extracted from patent WO2019201291A1 .

WM-8014 2 Publications Verification	Histone Acetyltransferase	Cancer
WM-8014 is an inhibitor of MOZ, a member of **histone acetyltransferases, with an IC₅₀** of 55 nM.

MOZ-IN-2	Histone Acetyltransferase	Cancer
MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC₅₀ of 125 μM.

SYY-B085-1	Histone Acetyltransferase	Cancer
SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor extracted from patent WO2019201291A1 .

HY-143441

CBP/p300-IN-17	Histone Acetyltransferase	Cancer
CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively .

HY-143442

CBP/p300-IN-18	Histone Acetyltransferase	Cancer
CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively .

HY-143440

CBP/p300-IN-16	Histone Acetyltransferase	Cancer
CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively .

HY-134964

CTB 3 Publications Verification	Histone Acetyltransferase Apoptosis	Neurological Disease Cancer
CTB is a potent p300 histone acetyltransferase activator . CTB can effectively induce apoptosis in MCF-7 cells .

HY-154944

JG-2016

Histone Acetyltransferase Cancer

JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1), with an IC₅₀ of 14.8 μM in the HAT1 acetylation assays .

JG-2016	Histone Acetyltransferase	Cancer
JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1), with an IC₅₀ of 14.8 μM in the HAT1 acetylation assays .

HY-N0005

Curcumin Maximum Cited Publications 62 Publications Verification Diferuloylmethane; Natural Yellow 3; Turmeric yellow	Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis	Cancer
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

HY-W015239

KAT8-IN-1	Others	Inflammation/Immunology Cancer
KAT8-IN-1 is a *lysine (K) acetyltransferase* 8 (KAT8) inhibitor, with IC₅₀s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8** inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases .

HY-N2020

Anacardic Acid 5+ Cited Publications Hydroginkgolic acid; Ginkgolic Acid C15:0	Histone Acetyltransferase Epigenetic Reader Domain Bacterial	Cancer
Anacardic Acid, extracted from cashew nut shell liquid, is a **histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC₅₀**s of ∼8.5 μM and ∼5 μM, respectively.

HY-114566

SPV106	Histone Acetyltransferase	Metabolic Disease
SPV106 is histone acetylase (HAT) and GCN5-related N-acetyltransferases (GNAT) activator. SPV106 can be used for the research of type 2 diabetes (T2D) .

HY-128876

CBP/p300-IN-3

Histone Acetyltransferase Cancer

CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1 .

CBP/p300-IN-3	Histone Acetyltransferase	Cancer
CBP/p300-IN-3, a p300/CBP **histone acetyltransferase** inhibitor, Compound 6, is sourced from patent WO 2019049061 A1 .

HY-107455

A-485 40+ Cited Publications	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively .

HY-136285

CPI-1612	Histone Acetyltransferase	Cancer
CPI-1612 is a highly potent, orally active *EP300/CBP histone* acetyltransferase (HAT) inhibitor with an IC₅₀ of 8.1 nM for EP300 HAT**. CPI-1612 has an anticancer activity .

HY-128875

CBP/p300-IN-10	Histone Acetyltransferase	Cancer
CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC₅₀ values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer .

HY-100132

CBP/p300-IN-5	Histone Acetyltransferase	Cancer
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC₅₀ of 18.8 nM .

HY-162128

Antitumor agent-130	Histone Acetyltransferase	Cancer
Antitumor agent-130 (Compound 7b) is a p300 histone acetyltransferases (HAT) inhibitor with an IC₅₀ of 1.51 μM. Antitumor agent-130 combinates with doxorubicin (HY-15142A) can significantly inhibit tumor growth and invasion in vitro and in vivo .

HY-139149

NiCur	Histone Acetyltransferase	Cancer
NiCur is a potent and selective *CBP histone* acetyltransferase (HAT) inhibitor with an IC₅₀ value of 0.35 μΜ. NiCur, which blocks CBP HAT** activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins .

HY-147290

NSC 694623	Histone Acetyltransferase	Cancer
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC₅₀ value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer .

HY-16531

YF-2 2 Publications Verification	Histone Acetyltransferase	Neurological Disease Cancer
YF-2 is a highly selective, blood-brain-barrier permeable **histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC₅₀**s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .

HY-16531A

YF-2 hydrochloride 2 Publications Verification	Histone Acetyltransferase	Neurological Disease Cancer
YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable **histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC₅₀**s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .

HY-110127

NU9056 3 Publications Verification	Histone Acetyltransferase Apoptosis	Cancer
NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells .

HY-117617

CAY10669	Histone Acetyltransferase	Cancer
CAY10669 (compound 6d) is an anacardic acid (HY-N2020) derivative that inhibits histone acetyltransferase PCAF with an IC₅₀ of 662 μM . CAY10669 enhances the SAHA-induced acetylation in HEPG2 cells, exhibits cytotoxicity in zebrafish embryo, promotes transgene expression in CHO-K1 cells .

HY-124696

PU139	Histone Acetyltransferase	Cancer
PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC₅₀s of 8.39, 9.74, 2.49 and 5.35 μM, respectively .

HY-145386

(S,S)-CPI-1612	Others	Cancer
(S,S)-CPI-1612 is the isomer of CPI-1612 (HY-136285), and can be used as an experimental control. CPI-1612 is a highly potent, orally active *EP300/CBP histone* acetyltransferase (HAT) inhibitor with an IC₅₀ of 8.1 nM for EP300 HAT**. CPI-1612 has an anticancer activity .

HY-136285A

(R,R)-CPI-1612	Others	Cancer
(R,R)-CPI-1612 is the isomer of CPI-1612 (HY-136285), and can be used as an experimental control. CPI-1612 is a highly potent, orally active *EP300/CBP histone* acetyltransferase (HAT) inhibitor with an IC₅₀ of 8.1 nM for EP300 HAT**. CPI-1612 has an anticancer activity .

HY-132197

CBP/p300-IN-12	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC₅₀ of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC₅₀ of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450 .

HY-100671

L002	Histone Acetyltransferase STAT	Inflammation/Immunology Cancer
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC₅₀ of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .

HY-107569

Garcinol 1 Publications Verification	Cholinesterase (ChE) Histone Acetyltransferase Apoptosis Endogenous Metabolite	Inflammation/Immunology Cancer
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 . 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 .

HY-149306

MS78	Histone Acetyltransferase MDM-2/p53	Cancer
MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .

HY-143443

DS17701585	Histone Acetyltransferase Histone Demethylase	Cancer
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC₅₀ values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research .

HY-143339

CBP/p300-IN-15	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC₅₀ values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC₅₀ values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research .

HY-138097

α-NETA 5+ Cited Publications	Chemerin Receptor Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis	Cancer
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity .

Histone Modification Research Compound Library	629 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 629 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

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Species:	Human (2)
Tag:	His (1) Tag Free (1)
Source:	E. coli (2)


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Histone acetyltransferase

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Recombinant Proteins

Antibodies

Natural
Products