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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. GC45483 Histone H3K9Me2 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    Histone H3 (3-17) (Lys9me2), H-Thr-Lys-Gln-Thr-Ala-Arg-Lys(Me2)-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-OH, Lys(Me2)9-Histone H3 (3-17), TKQTAR-K(Me2)-STGGKAPR

     A peptide fragment of histone H3
  3. GC45482 Histone H3K9Me1 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    Histone H3 (3-17) (Lys9me1), Lys(Me1)9-Histone H3 (3-17), TKQTAR-K(Me1)-STGGKAPR

     A peptide fragment of histone H3
  4. GC45481 Histone H3K79Me1 (69-89) amide (human, mouse, rat, bovine) (trifluoroacetate salt)

    Histone H3 (69-89) (Lys79me1) amide, Lys(Me1)79-Histone H3 (69-89) amide, RLVREIAQDF-K(Me1)-TDLRFQSSAV-NH2

     A peptide fragment of histone H3
  5. GC45480 Histone H3K4Me3 (1-25) amide (human mouse, rat, porcine, bovine) (trifluoroacetate salt)

    ART-K(Me3)-QTARKSTGGKAPRKQLATKAA-NH2, Histone H3 (1-25) (Lys4me3), H3K4me3, Lys(Me3)4-Histone H3 (1-25) amide

    A peptide fragment of histone H3
  6. GC45479 Histone H3K36Me3 (31-41) (trifluoroacetate salt)

    Histone H3 (31-41) (Lys36me3), Lys(Me3)36-Histone H3 (31-41), STGGV-K(Me3)-KPHRY

     A peptide fragment of histone H3
  7. GC45478 Histone H3K36Me3 (26-46)-K-biotin (trifluoroacetate salt)

    Histone H3 (26-46) (Lys36me3), Lys(Me3)36-Histone H3 (26-46)-K(Biotin), RKAAPATGGV-K(Me3)-KPHRYRPGTV-K(biotin)

     A peptide fragment of histone H3
  8. GC45477 Histone H3K14Ac/K18Ac/K23Ac/K27Ac (1-30)-GGK-biotin (trifluoroacetate salt)

    ARTKQTARKSTGG-K(Ac)-APR-K(Ac)-QLAT-K(Ac)-AAR-K(Ac)-SAPGG-K(biotin), Histone H3 (1-30) (Lys14ac/Lys18ac/Lys23ac/Lys27ac), Lys(Ac)14/18/23/27-Histone H3 (1-30)-GGK(biotin)

     A biotinylated fragment of histone H3
  9. GC45476 Histone H3K14Ac/H3K23Ac (1-24)-GGK-biotin (trifluoroacetate salt)

    ARTKQTARKSTGG-K(Ac)-APRKQLAT-K(Ac)-AGG-K(Biotin), Histone H3 (1-24) (Lys14ac/Lys23ac), Lys(Ac)14/23-Histone H3 (1-24)-GGK(Biotin)

     A biotinylated peptide fragment of histone H3
  10. GC45475 Histone H3 (1-35) (human, mouse, rat, bovine) (trifluoroacetate salt)

    ARTKQTARKSTGGKAPRKQLATKAARKSAPATGGV

     A peptide fragment of histone H3
  11. GC45474 Histone H3 (1-25) amide (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    ARTKQTARKSTGGKAPRKQLATKAA-NH2

     A peptide fragment of histone H3
  12. GC45402 CAY10729 (trifluoroacetate salt) (technical grade) A PAD1 inhibitor
  13. GC45389 BAY-6035 An inhibitor of SMYD3
  14. GC37971 ZM39923 A potent inhibitor of JAK3
  15. GC37966 ZINC13466751 ZINC13466751 是一种 HIF-1α/von Hippel-Lindau 相互作用的有效抑制剂，IC50 值为 2.0 ?M。
  16. GC37956 YUKA1 YUKA1 是一种有效、可透过细胞的赖氨酸脱甲基化酶 (KDM5A) 抑制剂，IC50 值为 2.66 μM，对 KDM5C 的作用较弱，IC50 值为 7.12 μM，对 KDM5B，KDM6A 或 KDM6B 无作用。YUKA1 可增加人细胞中 H3K4me3 的水平，具有抗肿瘤活性。
  17. GC37889 VCE-004.8

    VCE-?004.8

     VCE-004.8 (VCE-004.8) 是一种具有口服活性的特异性 PPARγ；和 CB2 受体双重激动剂。
  18. GC37881 Valemetostat tosylate

    DS-3201 tosylate

     Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂，用于复发/难治性周围 T 细胞淋巴瘤的研究。
  19. GC37856 UNC0321 A highly potent inhibitor of G9a histone methyltransferase
  20. GC37847 Tyk2-IN-8 Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
  21. GC37846 Tyk2-IN-7 Tyk2-IN-7 (Compound 48) 是 TYK2 JH2 抑制剂，与 TYK2 JH2 结构域结合，IC50 和 Ki.app 分别为 0.00053 μM 和 0.00007 μM。Tyk2-IN-7 (Compound 48) 是常规 TYK2 正构抑制剂的高选择性替代，抑制 TYK2/JAK1/JAK2 激酶结构域。Tyk2-IN-7 (Compound 48) 抑制小鼠 IL-12 诱导的 IFNγ 药效学模型中以及抑制在 IL-23 和 IL-12 依赖性小鼠结肠炎模型中的功效。
  22. GC37845 Tucidinostat

    西达本胺; Chidamide; HBI-8000; CS 055

     Tucidinostat，也称为Chidamide或CS055/HBI-8000，是HDAC1、HDAC2、HDAC3和HDAC10的抑制剂，IC50值分别为95 nM、160 nM、67 nM和78 nM。
  23. GC37801 TM6089 TM6089 是一种独特的 PHD 抑制剂，可刺激 HIF 活性而不会产生铁螯合作用，诱导血管生成并对缺血器官发挥保护作用。 TM6089 局部施用可增强血管生成，并且口服施用在表达缺氧反应的报告载体的转基因大鼠中刺激 HIF 活性。
  24. GC37761 Tenovin-6 Hydrochloride A small molecule activator of p53
  25. GC37753 Tefinostat

    CHR-2845

     Tefinostat (CHR-2845) 是一种单核细胞/巨噬细胞靶向的 HDAC 广谱抑制剂，通过细胞内酯酶人羧酸酯酶-1 (hCE-1) 切割成活性酸 CHR-2847。具有抗抗单核细胞系白血病活性。
  26. GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor
  27. GC37728 Talazoparib tosylate

    BMN 673ts

     Talazoparib tosylate（BMN 673ts）是一种有效的具有口服活性的PARP1/2抑制剂，是Talazoparib的甲苯磺酸盐形式。Talazoparib抑制PARP1的IC50值为0.57nM。
  28. GC37677 SRT 1720

    N-[2-[3-(1-哌嗪基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-喹喔啉甲酰胺

     A selective, potent SIRT1 activator
  29. GC37654 SMYD3-IN-1 SMYD3-IN-1 (compound 29) 是一种不可逆的、选择性的SMYD3 的抑制剂，其IC50 值为 11.7 nM。
  30. GC37651 SMI-16a

    PIM1/2 Kinase Inhibitor VI

     A Pim-1 kinase inhibitor
  31. GC37643 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
  32. GC37606 SCH-1473759 hydrochloride SCH-1473759 hydrochloride是多靶点的的极光激酶 (aurora) 抑制剂，对极光激酶A和B的IC50 值分别为4 和13 nM。
  33. GC37575 Ruxolitinib sulfate

    (BETAR)-BETA-环戊基-4-(7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-丙腈硫酸盐,INCB018424 sulfate

     A potent, selective JAK1/JAK2 inhibitor
  34. GC37523 RGB-286638 free base

    N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-C]吡唑-5-基]-N'-4-吗啉基脲

     A multi-kinase inhibitor
  35. GC37522 RGB-286638

    N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-C]吡唑-5-基]-N'-4-吗啉基脲盐酸盐

     A multi-kinase inhibitor
  36. GC37066 Rac-PT2399 Rac-PT2399 (Compound 10e) 是 PT2399 的消旋体，是一种有效且特异性的缺氧诱导因子 2a (HIF-2α) 抑制剂，IC50 为 0.01 μM。
  37. GC37034 PT2977

    PT2977; MK-6482

     PT2977 (Belzutifan, MK-6482), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).
  38. GC36975 Procyanidin B3

    原花青素 B3

     A polyphenol flavonoid dimer with diverse biological activities
  39. GC36969 PRMT5-IN-1 PRMT5 IN-1 是一种半缩醛胺，共价的蛋白质精氨酸甲基转移酶5 (PRMT5) 抑制剂，对 PRMT5/MEP50 的 IC50 为 11 nM。PRMT5 IN-1在生理条件下可以转化为醛并与 C449 反应形成共价加合物。
  40. GC36943 PNZ5 PNZ5 是一个有效的、异恶唑类的、BET 的广泛抑制剂，有着类似(+)-JQ1 的高选择性和强效作用，其对BRD4(1) 的KD 值为 5.43 nM。
  41. GC36918 PIM-447 dihydrochloride

    LGH447 dihydrochloride

     PIM447是泛PIM激酶抑制剂，对PIM1，PIM2，PIM3的 Ki 分别为6，18，9 nM。
  42. GC36905 PI3K/HDAC-IN-1 PI3K/HDAC-IN-1 是一种有效的 (PI3K/HDAC) 双重抑制剂，高效抑制 PI3Kδ 和 HDAC1 的 IC50 值分别为 8.1 nM 和 1.4 nM。
  43. GC36887 PF-CBP1 hydrochloride An inhibitor of the CBP and p300 bromodomains
  44. GC36882 PF-06263276 PF-06263276 (PF 6263276) 是一种有效、选择性的 pan-JAK 抑制剂，对 JAK1、JAK2、JAK3 和 TYK2 的抑制作用 IC50 值分别为 2.2 nM、23.1 nM、59.9 nM 和 29.7 nM。
  45. GC36855 Paris saponin VII

    重楼皂苷 VII; Chonglou Saponin VII

     Chonglou Saponin VII (Dioscinin, Polyphyllin-VII, Paris saponin-VII), a kind of steroidal saponins from Chonglou (Rhizoma Paridis Chonglou), inhibits EMT and reduces the invasion of ovarian cancer cells via the GSK-3β/β-catenin signaling pathway.
  46. GC36818 ORY-1001(trans)

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

     Iadademstat (ORY-1001) dihydrochloride 是一种选择性不可逆赖氨酸 (K) 特异性去甲基化酶 1A (KDM1A/LSD1) 抑制剂。
  47. GC36783 NVP-BSK805 dihydrochloride A potent, selective JAK2 inhibitor
  48. GC36751 NMS-P515 NMS-P515 是有效的、口服有效的、立体定向的PARP-1 的抑制剂，Kd 值为16 nM，IC50 值为 27 nM (Hela 细胞中)。有抗肿瘤活性。
  49. GC36738 Nicotinamide riboside chloride

    烟酰胺核糖氯酸盐

     A riboside form of nicotinamide
  50. GC36734 NI-42 An inhibitor of the BRPF1 bromodomain
  51. GC36691 Nanatinostat

    CHR-3996

     Nanatinostat (CHR-3996) 是一种有效的，有口服活性、I 类选择性的组蛋白去乙酰化酶 (HDAC) 抑制剂，IC50 值为 8 nM。

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