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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. GC62615 AS-99 AS-99 是一流的、有效的、选择性的 ASH1L 组蛋白甲基转移酶抑制剂（IC50=0.79μ；M，Kd=0.89μ；M），具有抗白血病活性。 AS-99 阻断细胞增殖，诱导细胞凋亡和分化，下调 MLL 融合靶基因，并减少体内白血病负担。
  3. GC62849 AS-99 TFA AS-99 TFA 是首创的、有效的、选择性的 ASH1L 组蛋白甲基转移酶抑制剂 (IC50= 0.79 µM, Kd= 0.89 µM)，具有抗白血病活性。AS-99 TFA 在体内阻断细胞增殖，诱导细胞凋亡 (apoptosis) 和分化，下调 MLL 融合靶基因，减轻白血病。
  4. GC17820 AS8351

    NSC51355

     A histone demethylase inhibitor
  5. GC10638 AT9283 A broad spectrum kinase inhibitor
  6. GC50066 Atiprimod dihydrochloride JAK2 inhibitor
  7. GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid
  8. GN10627 Atractylenolide I

    白术内酯 I

     A sesquiterpene with diverse biological activities
  9. GC64271 AU-15330 AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer.
  10. GC74035 AU-24118 AU-24118是mSWI/SNF ATP酶（SMARCA2和SMARCA4）和PBRM1的口服生物可利用蛋白水解靶向嵌合体（PROTAC）降解剂。
  11. GC39699 Aurintricarboxylic acid

    金精三羧酸

     A protein synthesis inhibitor with diverse biological activities
  12. GC72964 Aurkin A Aurkin A是极光A激酶（Aurora A Kinase，也称Aurka）与TPX2相互作用的变抗抑制剂，通过靶向TPX2结合位点，Kd为3.77 μM。
  13. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
  14. GC33379 Aurora B inhibitor 1 AuroraBinhibitor1是一种AuroraB(Aurora-1)抑制剂，Ki值<0.010uM。详细信息请参考专利文献WO2007059299A1中的化合物1-3。
  15. GC40667 Aurora Kinase Inhibitor II

    4-(4-Benzamidoanilino)-6,7-dimethoxyquinazoline

     Blocks Aurora A kinase activity
  16. GC15711 Aurora Kinase Inhibitor III A potent inhibitor of Aurora A kinase
  17. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8 是一种高选择性 Aurora 激酶的抑制剂。
  18. GC73375 Aurora Kinases-IN-3 Aurora Kinases-IN-3（化合物15a）是一种口服活性AURKB抑制剂，通过破坏AURKB的有丝分裂定位来引发AURKB抑制活性。
  19. GC13433 AZ 960

    5-氟-2-[[(1S)-1-(4-氟苯基)乙基]氨基]-6-[(5-甲基-1H-吡唑-3-基)氨基]-3-吡啶腈,AZ-960,AZ960

     A JAK2 inhibitor
  20. GC68711 AZ13824374 AZ13824374 是一种高效的选择性 ATAD2 抑制剂，对乳腺癌据抗增殖活性。AZ13824374 在 ATAD2 FRET 和 ATAD2 NanoBRET 检测中对 ATAD2 的 pIC50 分别为 8.2 和 6.2。
  21. GC65899 AZ3391 AZ3391 是一种有效的 PARP 抑制剂。AZ3391 是一种喹喔啉衍生物。PARP 酶家族在许多细胞过程中发挥重要作用，例如复制、重组、染色质重塑和 DNA 损伤修复。AZ3391具有研究中枢神经系统组织中发生的疾病和病症的潜力，例如大脑和脊髓 (信息摘自专利 WO2021260092A1，化合物 23)。
  22. GC13744 AZ505

    N-环己基-3-(3,4-二氯苯乙基氨基)-N-[2-[[2-[5-羟基-3-氧代-3,4-二氢-2H-苯并[B][1,4]恶嗪-8-基]乙基]氨基]乙基]丙酰胺

     An inhibitor of SMYD2
  23. GC13103 AZ505 ditrifluoroacetate

    N-环己基-3-[[2-(3,4-二氯苯基)乙基]氨基]-N-[2-[[2-(3,4-二氢-5-羟基-3-氧代-2H-1,4-苯并恶嗪-8-基)乙基]氨基]乙基]丙酰胺二(2,2,2-三氟乙酸盐)

     An inhibitor of SMYD2
  24. GC64124 AZ506 AZ506 是有效的 SMYD2 抑制剂，IC50 为 17 nM。AZ506 抑制细胞中 SMYD2 甲基转移酶的活性，导致 SMYD2 介导的甲基化信号减少。
  25. GC16725 AZ6102

    REL-2-[4-[6-[(3R,5S)-3,5-二甲基-1-哌嗪基]-4-甲基-3-吡啶基]苯基]-3,7-二氢-7-甲基-4H-吡咯并[2,3-D]嘧啶-4-酮

     A TNKS1/2 inhibitor
  26. GC46900 AZ9482 A PARP inhibitor
  27. GC48971 AZD 1152 (hydrochloride)

    5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺二盐酸盐

     A prodrug for a potent Aurora B inhibitor
  28. GC13014 AZD 5153 A BRD4 inhibitor
  29. GC73919 AZD-9574-acid PPAR-1抑制剂AZD-9574-acid (70D)可用于合成PROTAC （CAS 2923686-70-6）。
  30. GC14709 AZD1152

    5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD-1152;AZD 1152

     AZD1152 (AZD1152) 是 AZD1152-hQPA 的前药，是一种高选择性的 Aurora B 抑制剂，在无细胞试验中 IC50 为 0.37 nM。 AZD1152 (AZD1152) 在癌细胞中诱导生长停滞和凋亡。
  31. GC12660 AZD1208

    AZD 1208;AZD-1208

     AZD1208 是一种有效、高选择性且可口服的 Pim 激酶抑制剂，对 PIM1、PIM2 和 PIM3 的 IC50 值分别为 0.4、5 和 1.9nM。
  32. GC35447 AZD1208 hydrochloride A pan-Pim kinase inhibitor
  33. GC12504 AZD1480

    5-氯-N2-[(1S)-1-(5-氟-2-嘧啶基)乙基]-N4-(5-甲基-1H-吡唑-3-基)-2,4-嘧啶二胺,AZD 1480

     AZD1480是一种JAK抑制剂（JAK1：IC50 = 1.3nM；JAK2：IC50 = 0.4nM） 。
  34. GC17965 AZD2461

    4-[4-氟-3-[(4-甲氧基哌啶-1-基)羰基]苄基]酞嗪-1(2H)-酮

     A PARP inhibitor
  35. GC35448 AZD5153 6-Hydroxy-2-naphthoic acid

    AZD5153结晶体(API形式),AZD-5153 HNT salt

     AZD-5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD-5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.
  36. GC62310 AZD5305

    AZD5305

     AZD5305 is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).
  37. GC14955 Barasertib (AZD1152-HQPA)

    5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34

     A selective Aurora kinase B inhibitor
  38. GC11572 Bardoxolone methyl

    甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester

     A synthetic triterpenoid with potent anticancer and antidiabetic activity
  39. GC14844 Baricitinib (LY3009104, INCB028050)

    巴瑞替尼; LY3009104; INCB028050

     A JAK1 and JAK2 inhibitor
  40. GC13830 Baricitinib phosphate

    磷酸巴瑞克替尼; LY3009104 phosphate; INCB028050 phosphate

     A JAK1 and JAK2 inhibitor
  41. GC73130 Basroparib

    STP1002

     Basroparib是一种具有抗肿瘤活性的强效聚ADP核糖聚合酶（PARP）抑制剂。
  42. GC12698 BAY 87-2243 A mitochondrial complex I inhibitor and inducer of ferroptosis
  43. GC18508 BAY-299 A potent and selective BRD1 inhibitor
  44. GC18159 BAY-598 An inhibitor of SMYD2
  45. GC45389 BAY-6035 An inhibitor of SMYD3
  46. GC33104 BAY1238097 BAY1238097是一种有效的、BET与组蛋白结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML(急性髓性白血病)和MM(多发性骨髓瘤)模型中表现出较强的抗增殖活性(TR-FRET中测得的IC50值<100nM)。
  47. GC91506 Bayer 18 Bayer 18 is a tyrosine kinase 2 (TYK2) inhibitor (IC50 = 18.7 nM).
  48. GC63694 BAZ1A-IN-1 BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
  49. GC15175 BAZ2-ICR A BAZ2A/B bromodomain inhibitor
  50. 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。
  51. GC35480 BB-Cl-Amidine hydrochloride A PAD4 inhibitor

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