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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Histone Acetyltransferases

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

    (R)(+)Etomoxir

     (R)-(+)-Etomoxir sodium salt(Etomoxir) is a small molecule developed for metabolic and cardiovascular disease that exhibits nanomolar potency toward CPT-1a and CPT-1b upon enzymatic conversion to the active inhibitor etomoxiryl CoA (IC50 = 0.01-0.70 µM). (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. GC42466 4-pentynoyl-Coenzyme A (trifluoroacetate salt)

    Click Tag 4pentynoylCoA

     Protein acetylation is a reversible, post-translational modification regulated by lysine acetyltransferases and deacetylases and plays a key role in regulating gene expression. 4-pentynoyl-Coenzyme A (trifluoroacetate salt) Chemical Structure
  5. GC32677 A-485 A-485 is a potent and selective p300/CBP (histone acetyltransferase paralog/CREB binding protein) catalytic inhibitor with IC50 of 60nM for p300 HAT. A-485 inhibits the activity of p300-BHC (bromodomain HAT-C/H3) and CBP-BHC domains with IC50 of 9.8nM and 2.6nM, respectively. A-485 Chemical Structure
  6. GC12917 Acetaminophen

    4-Acetamidophenol, APAP, 4'-Hydroxyacetanilide, NSC 3991, NSC 109028, Paracetamol

    A COX inhibitor

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

    histone acetyltransferase Gcn5 inhibitor

     Butyrolactone 3 Chemical Structure
  9. 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
  10. 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
  11. 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
  12. GC68841 CBP/p300-IN-10

    CBP/p300-IN-10 is an efficient inhibitor of histone acetyltransferases EP300 and CREBBP, with IC50 values of 26 nM and 39 nM, respectively.

     CBP/p300-IN-10 Chemical Structure
  13. GC73365 CBP/p300-IN-20 CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 Chemical Structure
  14. 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
  15. 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
  16. GC11539 CI 976

    PD 128042

     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
  17. 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
  18. GC10382 CPI-637 CBP/EP300 bromodomain inhibitor CPI-637 Chemical Structure
  19. 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
  20. GC14428 CPTH2 (hydrochloride) inhibitor of HAT activity of Gcn5 CPTH2 (hydrochloride) Chemical Structure
  21. GC43321 CPTH6 (hydrobromide) CPTH6 is a thiazole derivative that inhibits the lysine acetyltransferase activity of Gcn5 and pCAF but not p300 or CBP. CPTH6 (hydrobromide) Chemical Structure
  22. GC19891 CTB

    Cholera Toxin B subunit

    A potent p300 histone acetyltransferase activator

     CTB Chemical Structure
  23. GC14524 CTPB selective activator of the histone acetyltransferase (HAT) p300 CTPB Chemical Structure
  24. GC14787 Curcumin

    Indian Saffron, Turmeric yellow

     A yellow pigment with diverse biological activities Curcumin Chemical Structure
  25. 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
  26. 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
  27. 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
  28. GC73397 DS-9300 DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 Chemical Structure
  29. GC31245 EML 425 An inhibitor of p300 and CBP EML 425 Chemical Structure
  30. GC13474 Garcinol

    Camboginol

    Garcinol is an nonspecificity inhibitor of the histone acetyltransferases (HATs) p300 and PCAF .IC50 values are 7μM and 5μM respectively.

     Garcinol Chemical Structure
  31. 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
  32. 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
  33. 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
  34. 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
  35. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor GSK 4027 Chemical Structure
  36. 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
  37. GC12009 HAT Inhibitor II

    Histone Acetyltransferase 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
  38. GC33422 HAT-IN-1 HAT-IN-1 is an inhibitor of HAT, used in the research of cancer. HAT-IN-1 Chemical Structure
  39. GC43837 Histone H3 Peptide Substrate (1-21)

    H3 Peptide

     Histone H3 undergoes many modifications including acetylation, methylation, and phosphorylation that are important for regulation of gene transcription. Histone H3 Peptide Substrate (1-21) Chemical Structure
  40. 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
  41. GC50721 iP300w iP300w Chemical Structure
  42. GC15836 IWP 12

    Inhibitor of Wnt Production-12

     Potent inhibitor of Porcupine (PORCN) IWP 12 Chemical Structure
  43. GC73536 JET-209 JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 Chemical Structure
  44. GC73483 KAT modulator-1 KAT modulator-1 (Compound 3) is a KAT modulator. KAT modulator-1 Chemical Structure
  45. GC69326 KAT6-IN-1

    KAT6-IN-1 is an effective inhibitor of KAT6 and can be used for cancer research.

     KAT6-IN-1 Chemical Structure
  46. GC91622 KAT8 Inhibitor 19

    Lysine Acetyltransferase 8 Inhibitor 19

     KAT8 inhibitor 19 is an inhibitor of lysine acetyltransferase 8 (KAT8; IC50 = 12.1 µM). KAT8 Inhibitor 19 Chemical Structure
  47. GC45503 L-Moses (hydrochloride)

    L-45

       L-Moses (hydrochloride) Chemical Structure
  48. GC15731 L002

    p300/CBP Inhibitor VI, NSC 764414

     p300 inhibitor L002 Chemical Structure
  49. GC68405 Lys-CoA TFA Lys-CoA TFA Chemical Structure
  50. GC73460 MC4171 MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 Chemical Structure
  51. GC15049 MCB-613

    stimulator of steroid receptor coactivator (SRC)

     MCB-613 Chemical Structure
  52. GC11439 MG 149

    Tip60 HAT inhibitor

     HAT inhibitor MG 149 Chemical Structure
  53. GC33371 MOZ-IN-2 An inhibitor of KAT6A/MOZ MOZ-IN-2 Chemical Structure
  54. GC73228 MS78 MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 Chemical Structure
  55. 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
  56. GC18750 NEO2734

    EP31670

     An orally active dual p300/CBP and BET bromodomain selective inhibitor NEO2734 Chemical Structure
  57. 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
  58. 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
  59. 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
  60. GC14103 NSC228155 EGFR activator NSC228155 Chemical Structure
  61. 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
  62. 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
  63. GC62247 PF-9363

    CTx-648

     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
  64. 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
  65. GC36975 Procyanidin B3

    (+)-Catechin-(4α→8)-(+)-catechin, Proanthocyanidin B3, Procyanidol B3

     A polyphenol flavonoid dimer with diverse biological activities Procyanidin B3 Chemical Structure
  66. 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
  67. GC11430 Remodelin Remodelin is a small molecule inhibitor of N-acetyltransferase 10 (NAT10).Dysregulation of N-acetyltransferase 10 (NAT10) is associated with the development of many types of tumors. Remodelin Chemical Structure
  68. 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
  69. GC41638 TSI-01 TSI-01 is a selective inhibitor of lysophosphatidylcholine acyltransferase 2 (LPCAT2) with IC50 values of 0.47 and 3.02 µM for human LPCAT2 and LPCAT1, respectively. TSI-01 Chemical Structure
  70. GC45094 TTK21 TTK21 is an activator of CBP/p300 histone acetyltransferase activity. TTK21 Chemical Structure
  71. GC10931 VULM 1457 Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor VULM 1457 Chemical Structure
  72. GC18154 WM-1119

    A highly potent, selective KAT6A/B inhibitor

     WM-1119 Chemical Structure
  73. 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
  74. GC18153 WM-8014

    WM8014,WM 8014

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

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

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