1. Epigenetics
  2. Histone Acetyltransferase

Histone Acetyltransferase

The histone acetyltransferase (HAT) enzymes p300 and CBP are closely related paralogs that serve as transcriptional coactivators. The p300 and CBP catalyze the acetylation of Lys residues in histones and other proteins. Serving as transcriptional coactivators, p300 and CBP participate in numerous ways to regulate cell growth, differentiation, and gene expression across many organ systems and physiologic pathways. Dysregulation of p300/CBP by mutation, altered expression, or other mechanisms has been linked to disease states, including various malignancies such as acute leukemias and prostate cancer. Furthermore, p300/CBP is critical in development as evidenced by the genetic disorder Rubinstein-Taybi syndrome, which occurs with loss of function mutations in single alleles of either p300 or CBP.

Inhibitors of p300/CBP HAT activity have been developed and are under investigation as therapeutics for a number of diseases.

Histone Acetyltransferase 相关产品 (23):

Cat. No. Product Name Effect Purity
  • HY-107455
    A-485 Inhibitor 99.08%
    A-485 是 p300/CBP 的强效选择性催化抑制剂,对 p300CBPIC50 值分别为 9.8 nM 和 2.6 nM。
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin是一种天然酚类化合物,具有抗炎,抗氧化,抗增殖和抗血管生成等多种活性。 Curcumin是p300组蛋白乙酰转移酶 ((HATs)) 抑制剂,也显示对 NF-κBMAPKs 的抑制作用。
  • HY-13823
    C646 Inhibitor >98.0%
    C646 是选择性,竞争性的 histone acetyltransferase p300 抑制剂,Ki 值为 400 nM,对其他的乙酰转移酶作用较小。
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637是一个强的和有选择性的CBP/EP300 bromodomains的抑制剂,在CBP/EP300 和 BRD4中的IC50分别是 0.03±0.01μM 和 11.0±0.6 μM。
  • HY-15826
    SGC-CBP30 Inhibitor 99.19%
    SGC-CBP30是CREBBP和EP300的布罗莫结构域抑制剂,IC50分别为21-69nM和38 nM。
  • HY-102058
    WM-1119 Inhibitor >98.0%
    WM-1119 是强效的、KAT6A/B 的选择性抑制剂,其对 KAT6A 的 IC50 值为 0.25 μM,对 KAT6A,KAT5,KAT7的 KD 值分别为 2 nM,2.2 μM,0.5 μM。
  • HY-108696
    GNE-781 Inhibitor
    GNE-781 是一种高效的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50 为 0.94 nM。GNE-781 还抑制 BRETBRD4 (1)IC50 分别为 6.2 nM 和 5100 nM。
  • HY-101027
    GSK 4027 Inhibitor 98.01%
    GSK 4027 是一种 PCAF/GCN5 溴结构域的化学探针,作用于 PCAF,pIC50 为 7.4±0.11。
  • HY-15887
    MG 149 Inhibitor 99.48%
    MG149是Tip60抑制剂,IC50为74 uM,对MOF的抑制性较相似,IC50为47 uM,而对PCAF和p300则几乎无活性。
  • HY-100726
    GNE-272 >98.0%
    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 13 μM。
  • HY-19541
    I-CBP112 Inhibitor 98.57%
    I-CBP112是一种特异性和有效的乙酰-赖氨酸竞争性蛋白-蛋白相互作用抑制剂,靶向CBP/p300溴结构域, 在白血病细胞中的IC50值为5.5±1.1 μM。
  • HY-N2020
    Anacardic Acid Inhibitor >98.0%
    Anacardic Acid 是从从腰果壳中提取液中分离到的酸类物质,为 histone acetyltransferases 抑制剂,对 p300 和 PCAF 的 IC50 值分别为 ∼8.5 μM 和 ∼5 μM。
  • HY-19999A
    PF-CBP1 hydrochloride Inhibitor 99.77%
  • HY-100734
    Histone Acetyltransferase Inhibitor II Inhibitor 99.05%
    Histone Acetyltransferase Inhibitor II 是一种有效的,细胞渗透的 p300 抑制剂,IC50 值为 5 µM,可用于癌症研究。
  • HY-102060
    MOZ-IN-3 Inhibitor 99.70%
    MOZ-IN-3 是一种 MOZ (属于 histone acetyltransferases) 的抑制剂,IC50 值为 55 nM。
  • HY-100697
    TPOP146 Inhibitor 99.66%
    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134 nM和5.02 μM。
  • HY-16706A
    Remodelin hydrobromide Inhibitor 99.16%
  • HY-108435
    GNE-049 Inhibitor
    GNE-049 是一种高效的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50 为 1.1 nM。GNE-049 还抑制 BRETBRD4 (1)IC50 分别为 12 nM 和 4200 nM。
  • HY-16706
    Remodelin Inhibitor
  • HY-102059
    MOZ-IN-2 Inhibitor
    MOZ-IN-2 是 MOZ (属于 histone acetyltransferases) 的抑制剂,其IC50 值为125 μM。
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