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

Histone Acetyltransferases(组蛋白乙酰转移酶)

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.

  1. Cat.No. 产品名称 Information
  2. GC69669 PCAF-IN-2 PCAF-IN-2 (compound 17) 是一种有效的 PCAF 抑制剂，IC50 值为 5.31 µM。PCAF-IN-2 显示出抗肿瘤活性。CAF-IN-2 诱导细胞凋亡 (apoptosis) 和细胞周期阻滞在 G2/M 期。
  3. GC69597 NSC 694623 NSC 694623 是一种有效的组蛋白乙酰转移酶 (HAT) 抑制剂，对重组 HAT p300/CBP 相关因子 (PCAF) 的 IC50 为 15.9 μM。NSC 694623 对某些癌细胞具有抗增殖活性。NSC 694623 可用于抗癌研究。
  4. GC69326 KAT6-IN-1 KAT6-IN-1 是一种有效的 KAT6 抑制剂。KAT6-IN-1可用于癌症研究。
  5. GC68841 CBP/p300-IN-10 CBP/p300-IN-10 是一种高效的组蛋白乙酰转移酶 EP300 和 CREBBP 的抑制剂，IC50 分别为 26 nM 和 39 nM。
  6. GC68405 Lys-CoA TFA Lys-CoA TFA 是一种选择性 p300 组蛋白乙酰转移酶 (HAT) 抑制剂 (IC50=50-500 nM)。Lys-CoA TFA 对 p300 的选择性是 PCAF 的 100 多倍 (IC50=200 μM)。Lys-CoA TFA 抑制 p300-HAT 活性依赖的转录激活。
  7. GC66049 NSC 694621 NSC 694621 是一种有效的 PCAF 抑制剂，其 IC50 值为 5.71 µM (PCAF/H31-21)。NSC 694621 具有较好的抗癌活性，能抑制癌细胞的增殖。
  8. GC64137 Acetaminophen-d3 Acetaminophen-d3 (Paracetamol-d3) 是 Acetaminophen 的氘代物。Acetaminophen (Paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。Acetaminophen 是广泛使用的解热和止痛剂。
  9. GC63627 DCH36_06 DCH36_06 是一种有效的选择性 p300/CBP 抑制剂，对 p300 和 CBP 的 IC50 分别为 0.6 μM 和 3.2 μM。DCH36_06 介导的 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化。抗肿瘤活性。
  10. GC63405 PU139 PU139 是一种有效的泛组蛋白乙酰转移酶 (HAT) 抑制剂。PU139 阻断 HATs Gcn5、p300/CBP 相关因子 (PCAF)、CBP 和 p300，IC50 分别为 8.39、9.74、2.49 和 5.35 μM。
  11. GC62669 CPI-1612 CPI-1612 是一种高效的具有口服活性的 EP300/CBP 组蛋白乙酰转移酶 (HAT) 抑制剂，对于 EP300 HAT 的 IC50 值为 8.1 nM。CPI-1612 具有抗癌活性。
  12. GC62248 NiCur NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter.
  13. GC62247 PF-9363 PF-9363 (CTx-648) is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models.
  14. GC62104 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
  15. GC61841 Naphthol AS-E Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。
  16. GC50721 iP300w Potent p300/CBP inhibitor
  17. GC39365 CPTH2 A HAT inhibitor
  18. GC38469 CBP/p300-IN-3 P300/CBP-IN-3, a p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂，化合物 6，来源于专利 WO 2019049061 A1。
  19. GC36975 Procyanidin B3 A polyphenol flavonoid dimer with diverse biological activities
  20. GC36887 PF-CBP1 hydrochloride An inhibitor of the CBP and p300 bromodomains
  21. GC45094 TTK21 An activator of CBP/p300 histone acetyltransferase activity
  22. GC43192 CAY10685 A “clickable” analog of CPTH2
  23. GC41984 1-Alaninechlamydocin An HDAC inhibitor
  24. GC41638 TSI-01 A LPCAT2 inhibitor
  25. GC40767 CAY10669 An inhibitor of PCAF
  26. GC40226 Curcumin-d6 An internal standard for the quantification of curcumin
  27. GC34078 I-CBP112 A p300 and CBP inhibitor
  28. GC33422 HAT-IN-1 HAT-IN-1是HAT的抑制剂，用于癌症研究。
  29. GC33371 MOZ-IN-2 An inhibitor of KAT6A/MOZ
  30. GC33212 GNE-207 GNE-207是一种有效、选择性、可口服的CBP溴结构域抑制剂，IC50值为1nM，对其选择性是的BRD4(1)的2500多倍，IC50值为3.1μM。在MV-4-11细胞中，GNE-207对MYC表达具有高效活性，EC50值为18nM。
  31. GC33028 CF53 CF53是一种高效、选择性、可口服的BET抑制剂，对BRD4BD1的Ki值为<1nM，Kd值为2.2nM，IC50值为2nM；CF53对BRD2，BRD3，BRD4和BRDTBET蛋白的BD1和BD2两个结构域都有高亲和性，对其选择性远高于非含溴结构域BET蛋白。CF53在体外和体内都具有显著的抗肿瘤活性[1]
  32. GC32960 GNE-049 GNE-049是一种高效的选择性CBP抑制剂，在TR-FRET实验中IC50为1.1nM。GNE-049还抑制BRET和BRD4(1)，IC50分别为12nM和4200nM。
  33. GC32880 TPOP146 TPOP146是选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的Kd值分别为134nM和5.02μM。
  34. GC32747 GNE-272 GNE-272是有效和选择性的CBP/EP300溴结构域体内探针，对CBP，EP300和BRD4的IC50值分别为0.02，0.03和13μM。
  35. GC32677 A-485 A p300/CBP inhibitor
  36. GC32081 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
  37. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor
  38. GC31245 EML 425 An inhibitor of p300 and CBP
  39. GC31099 YF-2 A HAT activator
  40. GC30714 GSK4028 GSK4028是GSK4027的对映体阴性对照，GSK4027是一种PCAF/GCN5溴结构域的化学探针，而GSK4028对应的pIC50值为4.9。
  41. GC18154 WM-1119 An inhibitor of KAT6A
  42. GC18153 WM-8014 An inhibitor of KAT6A and KAT6B
  43. GC14524 CTPB A selective activator of p300 HAT
  44. GC12009 HAT Inhibitor II An inhibitor of HAT p300
  45. GC10226 Butyrolactone 3 A HAT inhibitor
  46. GC14428 CPTH2 (hydrochloride) A HAT inhibitor
  47. GC14103 NSC228155 An EGFR activator and inhibitor of KID-KIX interactions
  48. GC10382 CPI-637 An inhibitor of CBP/EP300 bromodomains
  49. GC15049 MCB-613 A small molecule stimulator of SRCs
  50. GC13474 Garcinol A polyisoprenylated benzophenone with diverse biological activities
  51. GC15836 IWP 12 A PORCN inhibitor

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