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Histone Methyltransferase(组蛋白甲基转移酶)

Histone methyltransferases are a group of enzymes that catalyze the methylation of histone lysine and arginine by adding methyl groups to specific histone arginine or lysine residues. Histone methyltransferaes can be classified into 3 classes, including SET domain lysine methyltransferases, non-SET domain lysine methyltransferases and arginine methyltransferases (PRMTs), all of which use S-adenosylmethionine as a cosubstrate for the transfer of the methyl group. Aberrant histone methylation has been associated with a wide range of human cancers (such as hematological malignancies), which leads to the development of novel cancer chemotherapies targeting cancer-associated histone methyltransferases (more than 20 lysine methyltransferases and 9 arginine methyltransferases in humans).

Products for  Histone Methyltransferase

  1. Cat.No. 产品名称 Information
  2. GC16015 A 366 A potent inhibitor of G9a
  3. GC10259 BRD4770

    HMTase Inhibitor VI

    An inhibitor of EHMT2/G9a
  4. GC10021 CPI-360 A selective EZH2 inhibitor
  5. GC17956 PFI-2

    (R)-PFI-2

    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride 是一种有效的选择性 SET 结构域,含有赖氨酸甲基转移酶 7 (SETD7) 抑制剂。
  6. GC16741 UNC0379 A selective SET8 inhibitor
  7. GC14249 UNC 0642

    2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺

    A G9a histone methyltransferase inhibitor
  8. GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor
  9. GC17672 TC-E 5003

    N,N'-[磺酰基二(4,1-亚苯基)]二(2-氯乙酰胺)

    A PRMT1 inhibitor
  10. GC11340 (R)-PFI 2 hydrochloride

    (R)-PFI-2 hydrochloride

    A SET7/9 inhibitor
  11. GC16599 CPI-169 A selective EZH2 inhibitor
  12. GC15259 EPZ004777 HCl EPZ004777 HCl 是一种有效的选择性 DOT1L 抑制剂,IC50 为 0.4 nM。
  13. GC14756 EI1

    6-氰基-N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-1-(1-乙基丙基)-1H-吲哚-4-甲酰胺,KB-145943

    A selective inhibitor of EZH2
  14. 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
  15. 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
  16. GC12548 UNC 0631 An inhibitor of G9a/GLP methyltransferases
  17. GC14364 SGI-1027

    DNA Methyltransferase Inhibitor II

    A DNA methyltransferase inhibitor
  18. GC11375 UNC1999 A selective, cell-permeable EZH2 inhibitor
  19. GC14652 MM-102

    HMTase Inhibitor IX

    An inhibitor of WDR5/MLL interactions
  20. GC18096 UNC669 A selective MBT inhibitor
  21. GC14062 EPZ-6438

    E-7438,Tazemetostat

    EPZ-6438 是一种有效且具有生物利用度的 EZH2 抑制剂,EZH2 是多梳抑制复合物 2 (PRC2) 的催化亚基,可催化组蛋白 H3 (H3K27) 的赖氨酸 27 甲基化,从而抑制含有人 PRC2 的活性抑制常数 Ki 值为 2.5 nM 的野生型 EZH2。

  22. GC15688 UNC 0224 A potent inhibitor of G9a histone methyltransferase
  23. GC16256 BVT 948

    4-羟基-3,3-二甲基-2H-苯并[G]吲哚-2,5(3H)-二酮

    An inhibitor of protein tyrosine phosphatases
  24. GC16518 UNC 0646

    N-(1-环己基-4-哌啶基)-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺

    An inhibitor of G9a/GLP methyltransferases
  25. GC14936 Chaetocin

    毛壳素

    据报道毛壳素是组蛋白甲基转移酶 (HMT)(例如 SUV39H1)的非特异性抑制剂,从而影响基因表达。
  26. GC16794 UNC1215

    UNC 1215;UNC-1215

    Potent L3MBTL3 domain inhibitor
  27. GC17534 GSK343

    GSK-343;GSK 343

    A selective, cell-permeable EZH2 inhibitor
  28. GC15783 GSK126

    EZH2 inhibitor;GSK-126;GSK 126

    GSK126(GSK2816126A, GSK2816126)是一种高选择性EZH2甲基转移酶抑制剂,在体外的IC50为12.6~17.4nM;在体内的IC50为9.9nM。
  29. GC13383 EPZ004777 EPZ004777 作为一种有效的表观遗传调节剂,可以逆转 TGF-β1 诱导的 T 调节细胞,可用于治疗多种免疫疾病。
  30. GC11491 SGC 0946 A potent inhibitor of DOT1L
  31. GC13878 EPZ005687

    EPZ 005687,EPZ-005687

    A potent, selective inhibitor of EZH2
  32. GC17334 Entacapone

    恩他卡朋

    Entacapone是一种有效的、可逆的、外周作用和具有口服活性的儿茶酚-O-甲基转移酶(COMT)抑制剂,可有效抑制大鼠肝脏总COMT,IC50和Ki值分别为20.1nM和10.7nM。
  33. GC12932 EPZ5676

    (2R,3R,4S,5R)-2-(6-氨基-9H-嘌呤-9-基)-5-((((1R,3S)-3-(2-(6-(叔丁基)-1H-苯并[D]咪唑-2-基)乙基)环丁基)(异丙基)氨基)甲基)四氢呋喃-3,4-二醇,EPZ-5676

    A highly potent DOT1L inhibitor
  34. GC17907 3-Deazaneplanocin A (DZNep) hydrochloride

    3-去氮腺嘌呤A盐酸盐; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    3-Deazaneplanocin A (DZNep) hydrochloride 是一种腺苷类似物,是一种竞争性 S-腺苷高半胱氨酸水解酶抑制剂,在无细胞试验中的 Ki 为 50 pM。
  35. GC15610 UNC0638 A G9a and GLP histone methyltransferase inhibitor
  36. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase
  37. GC17275 AMI-1

    猩红酸钠盐,Arginine N - methyltransferase inhibitor - 1

    A cell permeable inhibitor of PRMTs
  38. GC13145 3-Deazaneplanocin,DZNep

    3-去氮腺嘌呤A; DZNep; 3-Deazaneplanocin

    An inhibitor of lysine methyltransferase EZH2

  39. GP10020 Histone-H2A-(107-122)-Ac-OH

    Ac-Gly-Val-Leu-Pro-Asn-Ile-Gln-Ala-Val-Leu-Leu-Pro-Lys-Lys-Thr-Glu-OH

    Histone-H2A peptide

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