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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

  1. Cat.No. Product Name Information
  2. 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. (R)-(+)-Etomoxir sodium salt  Chemical Structure
  3. GC41984 1-Alaninechlamydocin 1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp. 1-Alaninechlamydocin  Chemical Structure
  4. GC32677 A-485 A p300/CBP inhibitor A-485  Chemical Structure
  5. GC12917 Acetaminophen

    A COX inhibitor

    Acetaminophen  Chemical Structure
  6. GC64137 Acetaminophen-d3 Acetaminophen-d3  Chemical Structure
  7. GC10226 Butyrolactone 3

    histone acetyltransferase Gcn5 inhibitor

    Butyrolactone 3  Chemical Structure
  8. 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.. C646  Chemical Structure
  9. 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. CAY10669  Chemical Structure
  10. 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. CAY10685  Chemical Structure
  11. GC38469 CBP/p300-IN-3 CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1. CBP/p300-IN-3  Chemical Structure
  12. 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. CF53  Chemical Structure
  13. 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. CI 976  Chemical Structure
  14. 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. CPI-1612  Chemical Structure
  15. GC10382 CPI-637 CBP/EP300 bromodomain inhibitor CPI-637  Chemical Structure
  16. 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). CPTH2  Chemical Structure
  17. GC14428 CPTH2 (hydrochloride) inhibitor of HAT activity of Gcn5 CPTH2 (hydrochloride)  Chemical Structure
  18. GC14524 CTPB selective activator of the histone acetyltransferase (HAT) p300 CTPB  Chemical Structure
  19. GC14787 Curcumin A yellow pigment with diverse biological activities Curcumin  Chemical Structure
  20. GC40226 Curcumin-d6 Curcumin-d6 is intended for use as an internal standard for the quantification of curcumin by GC- or LC-MS. Curcumin-d6  Chemical Structure
  21. 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. DCH36_06  Chemical Structure
  22. GC14490 Donepezil HCl Donepezil HCl (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil HCl  Chemical Structure
  23. GC31245 EML 425 An inhibitor of p300 and CBP EML 425  Chemical Structure
  24. GC13474 Garcinol

    Inhibitor of PCAF and p300 histone acetyltransferase (HAT) activity

    Garcinol  Chemical Structure
  25. 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. GNE-049  Chemical Structure
  26. 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. GNE-207  Chemical Structure
  27. 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. GNE-272  Chemical Structure
  28. 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. GNE-781  Chemical Structure
  29. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor GSK 4027  Chemical Structure
  30. 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. GSK4028  Chemical Structure
  31. 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. HAT Inhibitor II  Chemical Structure
  32. GC33422 HAT-IN-1 HAT-IN-1 is an inhibitor of HAT, used in the research of cancer. HAT-IN-1  Chemical Structure
  33. 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. I-CBP112  Chemical Structure
  34. GC50721 iP300w iP300w  Chemical Structure
  35. GC15836 IWP 12 Potent inhibitor of Porcupine (PORCN) IWP 12  Chemical Structure
  36. GC15731 L002 p300 inhibitor L002  Chemical Structure
  37. GC68405 Lys-CoA TFA Lys-CoA TFA  Chemical Structure
  38. GC15049 MCB-613

    stimulator of steroid receptor coactivator (SRC)

    MCB-613  Chemical Structure
  39. GC11439 MG 149 HAT inhibitor MG 149  Chemical Structure
  40. GC33371 MOZ-IN-2 An inhibitor of KAT6A/MOZ MOZ-IN-2  Chemical Structure
  41. 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. Naphthol AS-E  Chemical Structure
  42. 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. NiCur  Chemical Structure
  43. 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. NSC 694621  Chemical Structure
  44. 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.

    NSC 694623  Chemical Structure
  45. GC14103 NSC228155 EGFR activator NSC228155  Chemical Structure
  46. 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). NU 9056  Chemical Structure
  47. 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.

    PCAF-IN-2  Chemical Structure
  48. 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. PF-9363  Chemical Structure
  49. GC36887 PF-CBP1 hydrochloride PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 hydrochloride  Chemical Structure
  50. GC36975 Procyanidin B3 A polyphenol flavonoid dimer with diverse biological activities Procyanidin B3  Chemical Structure
  51. 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. PU139  Chemical Structure
  52. 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. Remodelin  Chemical Structure
  53. 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. TPOP146  Chemical Structure
  54. 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.

    TSI-01  Chemical Structure
  55. GC45094 TTK21 TTK21 is an activator of CBP/p300 histone acetyltransferase activity. TTK21  Chemical Structure
  56. GC10931 VULM 1457 Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor VULM 1457  Chemical Structure
  57. GC18154 WM-1119

    A highly potent, selective KAT6A/B inhibitor

    WM-1119  Chemical Structure
  58. 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. WM-3835  Chemical Structure
  59. GC18153 WM-8014

    Inhibitor for KAT6A (MOZ) and KAT6B (MORF/QKF), anticancer

    WM-8014  Chemical Structure
  60. GC31099 YF-2 A HAT activator YF-2  Chemical Structure
  61. GC12934 YM 750 Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor YM 750  Chemical Structure

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