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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. 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.
  3. GC39665 CMP-5 CMP-5 是一种有效的选择性 PRMT5 抑制剂，对 PRMT1，PRMT4 和 PRMT7 酶无活性。CMP-5 在组蛋白的准备过程中，通过抑制 PRMT5 甲基转移酶活性选择性地阻断 S2Me-H4R3。CMP-5 阻断 EBV 驱动的 B 淋巴细胞转化，但对正常 B 细胞没有影响。
  4. 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。
  5. GC39407 MS1943 A PROTAC that drives EZH2 degradation
  6. GC50576 MRK 740 Potent PRDM9 inhibitor
  7. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain
  8. GC50367 PF 06726304 acetate Highly potent and SAM-competitive EZH2 inhibitor
  9. GC50082 UNC 2399 UNC 2399 是一种生物素化的 UNC1999，是一种选择性 EZH2 降解剂，对 EZH2 保持高效的体外效力，IC50 为 17 nM。
  10. GC46213 Ro 41-0960 A COMT inhibitor
  11. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7
  12. GC45908 (R)-BAY-598 An inhibitor of SMYD2
  13. GC45763 Tolcapone-d4

    托卡朋-D4,Ro 40-7592-d4

     An internal standard for the quantification of tolcapone
  14. GC45609 ZLD1039 An inhibitor of EZH2
  15. GC38163 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat hydrobromide 抑制含有 PRC2 复合体的野生型 EZH2 的活性， Ki 值为 2.5±0.5 nM。Tazemetostat hydrobromide 抑制 EZH2，在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat hydrobromide 抑制大鼠 EZH2，IC50 为 4 nM。Tazemetostat hydrobromide 还抑制 EZH1，IC50 为 392 nM。
  16. GC38062 Gambogenic acid

    新藤黄酸

     Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
  17. GC45389 BAY-6035 An inhibitor of SMYD3
  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. 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。
  21. 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。
  22. GC36656 MS049 A selective, dual PRMT4/PRMT6 inhibitor
  23. GC36655 MS023 dihydrochloride An inhibitor of type I PRMTs
  24. GC36632 MM-102 TFA

    HMTase Inhibitor IX TFA

     An inhibitor of WDR5/MLL interactions
  25. GC36192 GSK3368715 dihydrochloride

    EPZ019997 dihydrochloride

     GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 是具有口服活性的，可逆的，SAM 非竞争性 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂 (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8))。GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 导致精氨酸甲基化状态的转变，改变了外显子的使用，具有很强的抗癌活性。
  26. GC36191 GSK3368715

    EPZ019997

     An inhibitor of type I PRMTs
  27. GC36168 GNA002 GNA002 是一种有效，选择性的，共价 EZH2 抑制剂，对 EZH2 的 IC50 为1.1 μM。GNA002 可以特异性，共价结合 EZH2-SET 结构域内的 Cys668，通过 Hsp70 相互作用蛋白 (CHIP) 介导的泛素化的 COOH 末端引发 EZH2 降解。GNA002 有效降低 EZH2 介导的 H3K27 三甲基化，重新激活 polycomb 阻遏复合物 2 (PRC2) 沉默的肿瘤抑制基因。
  28. GC36000 EPZ020411 hydrochloride A PRMT6 inhibitor
  29. GC35914 DW14800 DW14800 是一种蛋白精氨酸甲基转移酶 5 (PRMT5) 抑制剂，IC50 值为 17 nM。DW14800 降低 H4R3me2s 的水平，增强 HNF4α 的转录。抗肿瘤活性。
  30. GC35816 DC_C66 DC_C66 是一种细胞渗透性的，选择性的 (CARM1) 抑制剂，IC50 值为 1.8 μM。DC_C66 相对 PRMT1 (IC50=21 μM)，PRMT6 (IC50= 47μM)，PRMT5，具有良好的选择性。
  31. GC35742 CPUY074020 CPUY074020 是一种有效的 G9a 抑制剂，IC50 值为 2.18 μM，具有抗增殖活性。
  32. GC35714 CM-579 trihydrochloride CM-579 trihydrochloride 是一线的、可逆的，G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂，其IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。
  33. GC45117 UNC2327 An allosteric inhibitor of PRMT3
  34. GC44886 S-Farnesyl Thioacetic Acid

    FTA

     A competitive inhibitor of SAM-dependent methyltransferase
  35. GC44859 S-(5'-Adenosyl)-L-methionine chloride (hydrochloride)

    5'-[[(3S)-3-氨基-3-羧基丙基]甲基锍]-5'-脱氧腺苷氯化物二盐酸盐

    Ubiquitous methyl donor
  36. GC43837 Histone H3 Peptide Substrate (1-21)

    H3 Peptide

     Target substrate for several histone modifying enzymes
  37. GC43715 Furamidine (hydrochloride)

    呋喃脒二盐酸盐,DB75 dihydrochloride; NSC 305831 dihydrochloride

     A selective PRMT1 inhibitor and antiprotozoal agent
  38. GC43354 Cysmethynil

    Icmt Inhibitor

     An inhibitor of protein prenylation
  39. GC42944 BIX01294 (hydrochloride hydrate) An inhibitor of G9a histone methyltransferase
  40. GC42790 Amodiaquine

    阿莫地喹,Amodiaquin

     A prodrug form of N-desethyl amodiaquine
  41. GC42784 AMI-1 (sodium salt)

    Arginine N-Methyltransferase Inhibitor-1

     A cell permeable inhibitor of PRMTs
  42. GC41263 TP-064 A potent inhibitor of PRMT4
  43. GC34784 Sinefungin

    西奈芬净,Adenosyl-Ornithine; A-9145; Antibiotic 32232RP

    Sinefungin是病毒mRNA(鸟嘌呤-7-)-甲基转移酶、mRNA(核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。Sinefungin是一种SET7/9抑制剂，通过抑制H3K4甲基化来改善肾纤维化。
  44. GC34568 EHMT2-IN-2 EHMT2-IN-2是一种有效的EHMT抑制剂，对对EHMT1多肽,EHMT2多肽和细胞内EHMT2的IC50值均小于100nM。可用于血液疾病或癌症的研究。
  45. GC34567 EHMT2-IN-1 EHMT2-IN-1是一种有效的EHMT抑制剂，对EHMT1多肽,EHMT2多肽和细胞内EHMT2的IC50均小于100nM。用于血液疾病或癌症的研究。
  46. 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。
  47. GC34160 UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) A selective SET8 inhibitor
  48. GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

    EPZ-011989 trifluoroacetate

     An orally bioavailable EZH2 inhibitor
  49. GC34108 CARM1-IN-1

    Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor

     A selective inhibitor of PRMT4/CARM1
  50. GC33397 Valemetostat

    DS-3201

     A dual EZH1 and EZH2 inhibitor
  51. GC33320 CM-579 CM-579是一线的、可逆的，G9a和DNA甲基转移酶(DNMT)的双抑制剂，其IC50值分别为16nM和32nM。在多种癌细胞中发挥有效活性作用。

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