Histone Acetyltransferases
Histone acetyltransferases (HATs) are a diverse group of enzymes catalyzing a posttranslational modification of acetylation in which the acetyl group from the acetyl-CoA cofactor is transferred to the Nζ nitrogen of the target lysine side chain within histones. Based on the sequence divergence within the HAT domain, HATs is classified into at least five distinct families, including HAT1 family, Gcn5/PCAF family, MYST family, p300/CBP family and Rtt109 family. Despite the sequence divergence, a structurally conserved core region has been identified within each of the protein families, which contains a three-stranded β-sheet with a α—helix corresponding to the A and D regions of the Gcn5-related N-acetyltransferases (GNAT) proteins.
Products for Histone Acetyltransferases
- Cat.No. Product Name Information
- GC15104 (R)-(+)-Etomoxir sodium salt Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
- GC41984 1-Alaninechlamydocin 1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp.
- GC32677 A-485 A p300/CBP inhibitor
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GC12917
Acetaminophen
A COX inhibitor
- GC64137 Acetaminophen-d3
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GC10226
Butyrolactone 3
histone acetyltransferase Gcn5 inhibitor
- GC12733 C646 C646, a potent and selective p300/CBP histone acetyltransferase inhibitor (Ki 400 nM), has been shown to have pleiotropic activity, including neuroprotective, anti-cancer and anti-epithelial-mesenchymal transition (anti-EMT) effects..
- GC40767 CAY10669 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.
- GC43192 CAY10685 CAY10685 is a cell-active analog of the lysine acetyltransferase inhibitor CPTH2 that contains an alkyne moiety for use in click chemistry reactions.
- GC38469 CBP/p300-IN-3 CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
- GC33028 CF53 CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
- GC11539 CI 976 CI 976 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM.
- GC62669 CPI-1612 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.
- GC10382 CPI-637 CBP/EP300 bromodomain inhibitor
- GC39365 CPTH2 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).
- GC14428 CPTH2 (hydrochloride) inhibitor of HAT activity of Gcn5
- GC14524 CTPB selective activator of the histone acetyltransferase (HAT) p300
- GC14787 Curcumin A yellow pigment with diverse biological activities
- GC40226 Curcumin-d6 Curcumin-d6 is intended for use as an internal standard for the quantification of curcumin by GC- or LC-MS.
- GC63627 DCH36_06 DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
- GC14490 Donepezil HCl Donepezil HCl (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity.
- GC31245 EML 425 An inhibitor of p300 and CBP
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GC13474
Garcinol
Inhibitor of PCAF and p300 histone acetyltransferase (HAT) activity
- GC32960 GNE-049 GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
- GC33212 GNE-207 GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of?>2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
- GC32747 GNE-272 GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
- GC32081 GNE-781 GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.
- GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor
- GC30714 GSK4028 GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
- GC12009 HAT Inhibitor II HAT Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 μM. HAT Inhibitor II shows anti-acetylase activity in mammalian cells.
- GC33422 HAT-IN-1 HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
- GC34078 I-CBP112 I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
- GC50721 iP300w
- GC15836 IWP 12 Potent inhibitor of Porcupine (PORCN)
- GC15731 L002 p300 inhibitor
- GC68405 Lys-CoA TFA
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GC15049
MCB-613
stimulator of steroid receptor coactivator (SRC)
- GC11439 MG 149 HAT inhibitor
- GC33371 MOZ-IN-2 An inhibitor of KAT6A/MOZ
- GC61841 Naphthol AS-E Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 ?M), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 ?M. Naphthol AS-E can be used for cancer research.
- GC62248 NiCur 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.
- GC66049 NSC 694621 NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 μM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells.
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GC69597
NSC 694623
NSC 694623 is an effective inhibitor of histone acetyltransferase (HAT), with an IC50 of 15.9 μM against recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has anti-proliferative activity in certain cancer cells and can be used for anticancer research.
- GC14103 NSC228155 EGFR activator
- GC11972 NU 9056 Selective KAT5 (Tip60) histone acetyltransferase inhibitor (IC50 values are < 2, 60, 36, and >100 μM for KAT5, p300, pCAF and GCN5, respectively).
-
GC69669
PCAF-IN-2
PCAF-IN-2 (compound 17) is an effective inhibitor of PCAF, with an IC50 value of 5.31 μM. PCAF-IN-2 exhibits anti-tumor activity and induces apoptosis and cell cycle arrest at the G2/M phase.
- GC62247 PF-9363 PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.
- GC36887 PF-CBP1 hydrochloride PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD).
- GC36975 Procyanidin B3 A polyphenol flavonoid dimer with diverse biological activities
- GC63405 PU139 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.
- GC11430 Remodelin Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
- GC32880 TPOP146 TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
-
GC41638
TSI-01
Platelet-activating factor (PAF) is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli.
- GC45094 TTK21 TTK21 is an activator of CBP/p300 histone acetyltransferase activity.
- GC10931 VULM 1457 Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor
-
GC18154
WM-1119
A highly potent, selective KAT6A/B inhibitor
- GC62104 WM-3835 WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
-
GC18153
WM-8014
Inhibitor for KAT6A (MOZ) and KAT6B (MORF/QKF), anticancer
- GC31099 YF-2 A HAT activator
- GC12934 YM 750 Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor