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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. 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
  3. 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。
  4. 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.
  5. GC32052 Tyk2-IN-3 Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂，其IC50值为485nM。
  6. GC32028 BMS-066 BMS-066是IKKβ/Tyk2的抑制剂，其IC50值分别为9nM，72nM。
  7. GC32023 Abrocitinib (PF-04965842)

    PF-04965842(阿布罗替尼),PF-04965842

     A JAK1 inhibitor
  8. 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。
  9. 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.
  10. GC31887 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
  11. 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)。
  12. 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。
  13. 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。
  14. 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。
  15. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor
  16. GC31677 Oclacitinib maleate (PF-03394197 maleate)

    奥拉替尼马来酸盐; PF-03394197 maleate

     A JAK family kinase inhibitor
  17. 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。
  18. 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。
  19. GC31659 Tyk2-IN-4 (BMS-986165)

    BMS-986165

     An allosteric inhibitor of TYK2
  20. 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
  21. GC31511 Sinapinic acid (Sinapic acid)

    芥子酸; Sinapic acid

     A phenylpropanoid hydroxycinnamic acid with diverse biological activities
  22. GC31498 TP0463518 A pan HIF-PH inhibitor
  23. 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).
  24. GC31358 HIF-2α-IN-1 HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。
  25. GC31245 EML 425 An inhibitor of p300 and CBP
  26. 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。
  27. GC31099 YF-2 A HAT activator
  28. GC30922 SIRT2 Inhibitor II (AK-1) A SIRT2 inhibitor
  29. GC30782 ACY-775 An HDAC6 inhibitor
  30. 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.
  31. 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.
  32. 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。
  33. 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。
  34. GC30693 SIRT-IN-2 SIRT-IN-2是SIRT1/2/3的有效抑制剂，其IC50值分别为4，1，7nM。
  35. GC30644 INCB054329 Racemate INCB054329Racemate是BET蛋白的抑制剂。
  36. GC30601 Propanamide Propanamide 是一种从专利 WO2012122452A1 化合物 II 中提取的强效选择性 JAK 抑制剂，具有治疗皮肤疾病（如皮肤狼疮）的潜力。
  37. GC30530 Dot1L-IN-2 Dot1L-IN-2是一种有效的，选择性的，可口服的Dot1L(一种histonemethyltransferase)，IC50值和Ki值分别为0.4nM和0.08nM。
  38. GC30526 ACY-957 ACY-957是一种选择性的HDAC1和HDAC2抑制剂，对HDAC1/2/3的IC50值分别为7nM，18nM和1300nM，对HDAC4/5/6/7/8/9无作用。
  39. GC30503 A-893 A-893是一个有细胞活性的，SMYD2的抑制剂，其IC50值为2.8nM。
  40. GC30501 Lin28-let-7a antagonist 1 Lin28-let-7aantagonist1对Lin28-let-7a的结合有明显的拮抗作用，其对Lin28A-let-7a-1结合的IC50值为4.03μM。
  41. GC30263 Glucosamine (D-Glucosamine)

    氨基葡萄糖; D-Glucosamine; Chitosamine

     Glucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. Glucosamine（GS） treatment selectively downregulates HIF-1α at the protein level in YD-8 cells via interference of production of the citric acid cycle metabolites.
  42. GC30251 SIRT5 inhibitor SIRT5 inhibitor 是一种有效的 Human Sirtuin 5 deacylase 抑制剂，IC50 为 0.11 μM.
  43. GC30204 Sirtuin modulator 1 A SIRT1 activator
  44. GC19465 JNJ-64619178

    Onametostat

     A PRMT5 inhibitor
  45. GC19455 ZL0420 A BRD4 inhibitor
  46. GC18154 WM-1119 An inhibitor of KAT6A
  47. GC19419 PIM inhibitor 1 phosphate

    INCB053914 phosphate

     Uzansertib (INCB053914) phosphate 是一种具有口服活性的 ATP 竞争性泛 PIM 激酶抑制剂，对 PIM1、PIM2、PIM3 的 IC50 分别为 0.24 nM、30 nM、0.12 nM。 PIM inhibitor 1 phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。
  48. GC19410 NCGC00244536

    3-(8-羟基喹啉-6-基)-N-(3-苯基丙基)苯甲酰胺,KDM4B Inhibitor B3

     A KDM4B/JMJD2B inhibitor
  49. GC19409 ABBV-744 A BD2 bromodomain inhibitor
  50. GC19408 FM381 A potent JAK3 inhibitor
  51. GC19406 TH34 TH34 是一种 HDAC6/8/10 抑制剂，IC50 分别为 4.6 μM、1.9 μM 和 7.7 μM，对 HDAC1/2/3 具有高选择性。

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