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Home >> Signaling Pathways >> Chromatin/Epigenetics

Chromatin/Epigenetics(染色质/表观遗传学)

Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Products for  Chromatin/Epigenetics

  1. Cat.No. 产品名称 Information
  2. GC32798 MI-538 MI-538是menin和MLL融合蛋白相互作用的抑制剂；IC50值为21nM。
  3. GC32793 Rucaparib Camsylate

    瑞卡帕布樟脑磺酸盐,AG014699 camsylate; PF-01367338 camsylate

     A PARP1 inhibitor
  4. GC32791 BETd-260 (ZBC 260)

    ZBC 260

     BETd-260 (ZBC 260) (ZBC 260) 是一种 PROTAC，通过 Cereblon 和 BET 的配体连接，对 RS4;11 白血病细胞系中的 BRD4 蛋白具有低至 30 pM 的作用。 BETd-260 (ZBC 260) 在肝细胞癌 (HCC) 细胞中有效抑制细胞活力并强烈诱导细胞凋亡。
  5. GC32790 KDM5-IN-1 KDM5-IN-1是高效选择，有口服活性的KDM5抑制剂，IC50值为15.1nM。
  6. GC32764 GSK-LSD1 Dihydrochloride An LSD1 inhibitor
  7. GC32747 GNE-272 GNE-272是一种有效和选择性的环磷酸腺苷反应元件结合蛋白（CBP）抑制剂，是E1A结合蛋白p300（EP300）的抑制剂，IC50值分别为0.02和0.03μM，也是CBP/EP300溴结构域体内探针。
  8. GC32745 OSS_128167 OSS_128167是一种有效的选择性沉默调节蛋白6 (SIRT6)抑制剂，IC50为89 μM。
  9. GC32724 LW6 (HIF-1α inhibitor)

    HIF-1α inhibitor; LW8

     LW6是一种缺氧诱导因子1(hypoxia inducing factor 1, HIF)抑制剂,通过降解HIF-1α有效抑制HIF-1α的积累,但不影响缺氧时HIF- 1a mRNA水平。
  10. GC32719 dBET6 A PROTAC that drives BRD4 degradation
  11. GC32699 QC6352

    QC6352是一种有效的KDM4C抑制剂，其IC50值为35nM。
  12. GC32693 GSK3326595 (EPZ015938)

    EPZ015938

     A PRMT5 inhibitor
  13. GC32689 666-15

    Compound 3i

     666-15是一种选择性环磷酸腺苷反应元件结合蛋白（CREB）抑制剂，IC50值为0.081±0.04μM。
  14. GC32685 ARV-771 A PROTAC that drives BET family protein degradation
  15. GC32680 PT-2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
  16. GC32677 A-485 A-485是有效的选择性p300/CBP（组蛋白乙酰转移酶旁系同源物/CREB结合蛋白）的催化抑制剂，对p300 HAT的IC50值为60nM。A-485可抑制p300-BHC（溴域HAT-C/H3）和CBP-BHC结构域的活性，IC50分别为9.8nM和2.6nM。
  17. GC32565 CRA-026440 CRA-026440 是一种有效的广谱 HDAC 抑制剂。
  18. GC32449 Desidustat

    ZYAN1

     An inhibitor of HIF-PH
  19. GC32435 Targapremir-210

    TGP-210

     Targapremir-210是有效的miR-210抑制剂，作用于MDA-MB-231细胞系的IC50值为200nM。Targapremir-210通过和miR-210的发夹前体结构结合，进而抑制miRNA的成熟。
  20. GC32303 Streptonigrin (Bruneomycin)

    棕霉素,Bruneomycin

     A phenylpyridylquinoline with diverse biological activities
  21. GC32228 Tilorone dihydrochloride

    盐酸替洛隆；梯洛龙二盐酸盐；替洛隆二盐酸盐；盐酸梯洛龙

     An interferon-inducing antiviral agent
  22. GC32083 Acriflavine

    吖啶黄; Acriflavinium chloride 3,6-Acridinediamine mix

     Acriflavine是用于标记高分子量RNA的荧光染料。它也是一种局部防腐剂。
  23. 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.
  24. GC32052 Tyk2-IN-3 Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂，其IC50值为485nM。
  25. GC32028 BMS-066 BMS-066是IKKβ/Tyk2的抑制剂，其IC50值分别为9nM，72nM。
  26. GC32023 Abrocitinib (PF-04965842)

    PF-04965842(阿布罗替尼),PF-04965842

     Abrocitinib (PF-04965842)是一种口服活性且选择性的Janus激酶（JAK）抑制剂，对JAK1和JAK2的IC50值分别为29nM和803nM。
  27. GC31999 JAK-IN-1 JAK-IN-1是JAK1/2/3抑制剂，IC50分别为0.26，0.8和3.2nM。JAK-IN-1对JAK3的选择性比JAK1高。
  28. GC31902 JAK3-IN-6 Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
  29. GC31887 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
  30. GC31881 MS417 (GTPL7512)

    GTPL7512

    MS417 (GTPL7512) 是一种选择性 BET 特异性 BRD4 抑制剂，与 BRD4-BD1 和 BRD4-BD2 结合，IC50 分别为 30、46 nM 和 Kds 分别为 36.1、25.4 nM，对 CBP BRD 的选择性较弱 (IC50, 32.7 &#956 ;M)。
  31. GC31866 JAK inhibitor 1

    JAK inhibitor 1 是从专利 US20170121327A1 化合物实施例 283 中提取的 JAK 抑制剂。
  32. GC31831 BET-IN-1 BET-IN-1 是所有八个 BET 溴结构域的泛抑制剂，并且比其他具有代表性的含溴结构域的蛋白质具有选择性。
  33. GC31755 BB-Cl-Amidine BB-Cl-Amidine 是一种肽基精氨酸脱氨酶 (PAD) 抑制剂，常用于研究 PAD 功能。
  34. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor
  35. GC31677 Oclacitinib maleate (PF-03394197 maleate)

    奥拉替尼马来酸盐; PF-03394197 maleate

     A JAK family kinase inhibitor
  36. GC31668 TYK2-IN-2 TYK2-IN-2是TYK2的抑制剂，可用于炎症及自身免疫病的研究。
  37. GC31660 Delgocitinib (JTE-052)

    迪高替尼,JTE-052

     Delgocitinib (JTE-052) (JTE-052) 是一种特异性 JAK 抑制剂，对 JAK1、JAK2、JAK3 和 Tyk2 的 IC50 分别为 2.8、2.6、13 和 58 nM。
  38. GC31659 Tyk2-IN-4 (BMS-986165)

    BMS-986165

     An allosteric inhibitor of TYK2
  39. GC31654 KG-501 (Naphthol AS-E phosphate)

    色酚AS-E磷酸盐,Naphthol AS-E phosphate

     An inhibitor of the protein-protein interaction between CREB and KIX domains
  40. GC31511 Sinapinic acid (Sinapic acid)

    芥子酸; Sinapic acid

     A phenylpropanoid hydroxycinnamic acid with diverse biological activities
  41. GC31498 TP0463518 A pan HIF-PH inhibitor
  42. GC31365 γ-Oryzanol

    γ-谷维素

     Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
  43. GC31358 HIF-2α-IN-1 HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。
  44. GC31245 EML 425 An inhibitor of p300 and CBP
  45. GC31230 Dencichin (Dencichine)

    三七素; Dencichin; ODAP

     Dencichin是一种最初从三七中提取的非蛋白质氨基酸，可以抑制HIF-脯氨酰羟化酶2（PHD-2）的活性。
  46. GC31099 YF-2 A HAT activator
  47. GC30922 SIRT2 Inhibitor II (AK-1) A SIRT2 inhibitor
  48. GC30782 ACY-775 An HDAC6 inhibitor
  49. GC30766 Tranylcypromine hemisulfate (dl-Tranylcypromine hemisulfate)

    反苯环丙胺半硫酸盐; SKF 385 hemisulfate

     Tranylcypromine (Parnate) is an irreversible inhibitor of monoamine oxidase (MAO) with a rapid onset of activity.
  50. GC30763 Benzenebutyric acid (4-Phenylbutyric acid)

    4-苯基丁酸; 4-PBA; Benzenebutyric acid

    4-Phenylbutyric acid (4-PBA, Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
  51. GC30733 SIRT-IN-1 SIRT-IN-1是SIRT1/2/3的有效抑制剂，其IC50值分别为15，10，33μM。

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