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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Histone Methyltransferase

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. GC45908 (R)-BAY-598 An inhibitor of SMYD2
  3. GC70906 (R)-HH2853 (R)-HH2853是EZH2突变型抑制剂，对EZH2- y641f的IC50 <100 nM。
  4. GC11340 (R)-PFI 2 hydrochloride

    (R)-PFI-2 hydrochloride

     A SET7/9 inhibitor
  5. GC65045 (S)-MRTX-1719 (S)-MRTX-1719 (example 16-7) 是 MRTX-1719 的 S- 对映体。(S)-MRTX-1719 是一种 PRMT5/MTA 复合物抑制剂，其 IC50 为7070 nM。
  6. GC13634 (S)-PFI-2 (hydrochloride)

    (+)-PFI-2

     Negative control of (R)-PFI 2
  7. 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。
  8. GC13145 3-Deazaneplanocin,DZNep

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

    An inhibitor of lysine methyltransferase EZH2
  9. GC16015 A 366 A potent inhibitor of G9a
  10. GC32861 A-196 A selective inhibitor of SUV420H1 and SUV420H2
  11. GC33187 A-395 (A395) A-395 (A395) 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂，有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12)，IC50 为 18 nM。
  12. 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。
  13. GC73923 AC1Q3QWB

    AQB

     AC1Q3QWB通过中断HOTAAIR-EZH2相互作用上调CDKN1A和SOX17，并增强Tazemetostat在子宫内膜癌症中的疗效。
  14. GC16509 Adox

    腺苷二醛

     An irreversible inhibitor of SAH hydrolase
  15. GC17275 AMI-1

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

     A cell permeable inhibitor of PRMTs
  16. GC42784 AMI-1 (sodium salt)

    Arginine N-Methyltransferase Inhibitor-1

     A cell permeable inhibitor of PRMTs
  17. GC39840 AMI-1 free acid

    猩红酸

     AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
  18. GC17546 AMI5

    水溶伊红,Acid Red 87

     曙红 Y（二钠）是一种可溶性酸性红色染料分子。
  19. GC42790 Amodiaquine

    阿莫地喹,Amodiaquin

     A prodrug form of N-desethyl amodiaquine
  20. GC60579 Amodiaquine dihydrochloride

    盐酸阿莫地喹,Amodiaquin dihydrochloride

     A prodrug form of N-desethyl amodiaquine
  21. GC10905 Amodiaquine dihydrochloride dihydrate

    阿莫地喹盐酸盐; Amodiaquin dihydrochloride dihydrate

     A prodrug form of N-desethyl amodiaquine
  22. GC73278 Anticancer agent 126 Anticancer agent 126（化合物12）是一种具有抗癌作用的WDR5抑制剂。
  23. GC65918 AS-85 AS-85 是一种有效的 ASH1L 抑制剂 (IC50=0.6 µM) 具有抗白血病活性。AS-85 与 ASH1L SET 域结合，Kd 值为 0.78 µM。
  24. 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。
  25. 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。
  26. 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
  27. 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
  28. 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。
  29. GC18159 BAY-598 An inhibitor of SMYD2
  30. GC45389 BAY-6035 An inhibitor of SMYD3
  31. GC18161 BCI-121 An inhibitor of SMYD3
  32. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain
  33. GC39663 BI-9321 trihydrochloride BI-9321 trihydrochloride 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。
  34. GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT
  35. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase
  36. GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) 是一种组蛋白赖氨酸甲基转移酶抑制剂。
  37. GC42944 BIX01294 (hydrochloride hydrate) An inhibitor of G9a histone methyltransferase
  38. GC25159 BMF-219 BMF-219是一种高选择性和不可逆的menin抑制剂,在小鼠模型中具有良好的抑制效果 。
  39. GC63731 BRD0639 An inhibitor of the protein-peptide interaction between PRMT5 and PBM
  40. GC10259 BRD4770

    HMTase Inhibitor VI

     An inhibitor of EHMT2/G9a
  41. GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays
  42. 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
  43. GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor
  44. GC12005 C7280948 A PRMT1 inhibitor
  45. GC73615 CARM1 degrader-1 hydrochloride CARM1 degrader-1 hydrochloride是CARM1降解剂-1的盐酸盐形式。
  46. GC34108 CARM1-IN-1

    Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor

     A selective inhibitor of PRMT4/CARM1
  47. GC34424 CARM1-IN-1 hydrochloride CARM1-IN-1盐酸盐是CARM1高效选择性抑制剂，IC50值为8.6uM，对PRMT1和SET7抑制活性很抵。
  48. GC73386 CARM1-IN-3 CARM1-IN-3（化合物17b）是一种强效且选择性的共激活剂相关精氨酸金属转移酶（CARM1）抑制剂，CARM1和CARM3的IC50值分别为0.07、>25µM。
  49. GC73387 CARM1-IN-3 dihydrochloride CARM1-IN-3 dihydrochloride是一种强效且选择性的共激活剂相关精氨酸金属转移酶（CARM1）抑制剂，CARM1和CARM3的IC50值分别为0.07、>25µM。
  50. GC18949 CAY10677

    Icmt Inhibitor 15

     An inhibitor of protein prenylation
  51. 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。

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