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

Histone Methyltransferase

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. Product Name Information
  2. GC45908 (R)-BAY-598 An inhibitor of SMYD2 (R)-BAY-598 Chemical Structure
  3. GC11340 (R)-PFI 2 hydrochloride PFI-2 ((R)-(R)-PFI 2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI 2 hydrochloride Chemical Structure
  4. GC65045 (S)-MRTX-1719 (S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM. (S)-MRTX-1719 Chemical Structure
  5. GC13634 (S)-PFI-2 (hydrochloride) Negative control of (R)-PFI 2 hydrochloride (S)-PFI-2 (hydrochloride) Chemical Structure
  6. GC17907 3-Deazaneplanocin A (DZNep) hydrochloride An inhibitor of the lysine methyltransferase EZH2 3-Deazaneplanocin A (DZNep) hydrochloride Chemical Structure
  7. GC13145 3-Deazaneplanocin,DZNep

    An inhibitor of lysine methyltransferase EZH2

     3-Deazaneplanocin,DZNep Chemical Structure
  8. GC16015 A 366 G9a/GLP histone lysine methyltransferase inhibitor A 366 Chemical Structure
  9. GC32861 A-196 A selective inhibitor of SUV420H1 and SUV420H2 A-196 Chemical Structure
  10. GC33187 A-395 (A395) A-395 (A395) is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM. A-395 (A395) Chemical Structure
  11. GC30503 A-893 A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM. A-893 Chemical Structure
  12. GC16509 Adox Adox, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research. Adox Chemical Structure
  13. GC17275 AMI-1 A cell permeable inhibitor of PRMTs AMI-1 Chemical Structure
  14. GC39840 AMI-1 free acid AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding. AMI-1 free acid Chemical Structure
  15. GC17546 AMI5 Eosin Y (disodium) is a soluble acid red dye molecule. AMI5 Chemical Structure
  16. GC42790 Amodiaquine Amodiaquine is an aminoquinoline antimalarial compound. Amodiaquine Chemical Structure
  17. GC60579 Amodiaquine dihydrochloride Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride Chemical Structure
  18. GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor Amodiaquine dihydrochloride dihydrate Chemical Structure
  19. GC65918 AS-85 AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78μM. AS-85 Chemical Structure
  20. GC62615 AS-99 AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=0.79μM, Kd=0.89μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo. AS-99 Chemical Structure
  21. GC62849 AS-99 TFA AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=?0.79??M, Kd=?0.89??M) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo. AS-99 TFA Chemical Structure
  22. GC13744 AZ505 SMYD2 inhibitor,potent and selective AZ505 Chemical Structure
  23. GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor AZ505 ditrifluoroacetate Chemical Structure
  24. GC64124 AZ506 AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal. AZ506 Chemical Structure
  25. GC18159 BAY-598

    A potent and selective SMYD2 inhibitor

     BAY-598 Chemical Structure
  26. GC45389 BAY-6035   BAY-6035 Chemical Structure
  27. GC18161 BCI-121

    A substrate-competitive SMYD3 inhibitor?

     BCI-121 Chemical Structure
  28. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain BI 9321 Chemical Structure
  29. GC39663 BI-9321 trihydrochloride BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells. BI-9321 trihydrochloride Chemical Structure
  30. GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT Bisubstrate Inhibitor 78 Chemical Structure
  31. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase BIX 01294 Chemical Structure
  32. GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) is a histone lysine methyltransferase inhibitor. BIX-01338 hydrate (BIX01338 hydrate) Chemical Structure
  33. GC42944 BIX01294 (hydrochloride hydrate) The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. BIX01294 (hydrochloride hydrate) Chemical Structure
  34. GC63731 BRD0639 BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities. BRD0639 Chemical Structure
  35. GC10259 BRD4770 novel G9a(EHMT2) inhibitor BRD4770 Chemical Structure
  36. GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays BRD9539 Chemical Structure
  37. GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor C 21 Chemical Structure
  38. GC12005 C7280948 Novel PRMT1 inhibitor C7280948 Chemical Structure
  39. GC34108 CARM1-IN-1 A selective inhibitor of PRMT4/CARM1 CARM1-IN-1 Chemical Structure
  40. GC34424 CARM1-IN-1 hydrochloride CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). CARM1-IN-1 hydrochloride Chemical Structure
  41. GC18949 CAY10677 Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. CAY10677 Chemical Structure
  42. GC14936 Chaetocin Inhibitor of lys9-specific HMTs Chaetocin Chemical Structure
  43. GC18577 CID-2818500 An inhibitor of PRMT1 CID-2818500 Chemical Structure
  44. GC12367 CM-272 CM-272 is a first-in-class reversible dual inhibitor against G9a and DNMTs with IC50 values of 8 nM and 382 nM, respectively [1]. CM-272 Chemical Structure
  45. GC33320 CM-579 CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells. CM-579 Chemical Structure
  46. GC35714 CM-579 trihydrochloride CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells. CM-579 trihydrochloride Chemical Structure
  47. GC39665 CMP-5 CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected. CMP-5 Chemical Structure
  48. GC16298 CPI-1205 EZH2 inhibitor CPI-1205 Chemical Structure
  49. GC16599 CPI-169 EZH2 inhibitor CPI-169 Chemical Structure
  50. GC10021 CPI-360 EZH2 inhibitor CPI-360 Chemical Structure
  51. GC35742 CPUY074020 CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity. CPUY074020 Chemical Structure
  52. GC43354 Cysmethynil Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Cysmethynil Chemical Structure
  53. GC48967 D-Homoserine lactone An enantiomer of L-homoserine lactone D-Homoserine lactone Chemical Structure
  54. GC65186 DC-S239 DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity. DC-S239 Chemical Structure
  55. GC63662 DCLX069 DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 ?M. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects. DCLX069 Chemical Structure
  56. GC35816 DC_C66 DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5. DC_C66 Chemical Structure
  57. GC67863 DDO-2093 dihydrochloride DDO-2093 dihydrochloride Chemical Structure
  58. GC33208 Dot1L-IN-1 Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM. Dot1L-IN-1 Chemical Structure
  59. GC30530 Dot1L-IN-2 Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 Chemical Structure
  60. GC62613 Dot1L-IN-4 Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM. Dot1L-IN-4 Chemical Structure
  61. GC65962 Dot1L-IN-5 Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM. Dot1L-IN-5 Chemical Structure
  62. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7 DS-437 Chemical Structure
  63. GC35914 DW14800 DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity. DW14800 Chemical Structure
  64. GC33220 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively. EBI-2511 Chemical Structure
  65. GC19130 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. EED226 Chemical Structure
  66. GC67934 EEDi-5285 EEDi-5285 Chemical Structure
  67. GC34567 EHMT2-IN-1 EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer. EHMT2-IN-1 Chemical Structure
  68. GC34568 EHMT2-IN-2 EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer. EHMT2-IN-2 Chemical Structure
  69. GC14756 EI1 EZH2 inhibitor EI1 Chemical Structure
  70. GC17334 Entacapone A reversible COMT inhibitor Entacapone Chemical Structure
  71. GC47294 Entacapone-d10 An internal standard for the quantification of entacapone Entacapone-d10 Chemical Structure
  72. GC14062 EPZ-6438

    A EZH2 inhibitor,potent and selective

     EPZ-6438 Chemical Structure
  73. GC64343 EPZ-719 EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases. EPZ-719 Chemical Structure
  74. GC13383 EPZ004777 A potent inhibitor of DOT1L EPZ004777 Chemical Structure
  75. GC48980 EPZ004777 (formate) A potent inhibitor of DOT1L EPZ004777 (formate) Chemical Structure
  76. GC15259 EPZ004777 HCl EPZ004777 HCl is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM. EPZ004777 HCl Chemical Structure
  77. GC13878 EPZ005687 A potent, selective inhibitor of EZH2 EPZ005687 Chemical Structure
  78. GC19141 EPZ011989 EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase. EPZ011989 Chemical Structure
  79. GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) Chemical Structure
  80. GC15302 EPZ015666 PRMT5 inhibitor EPZ015666 Chemical Structure
  81. GC15102 EPZ020411 PRMT6 inhibitor EPZ020411 Chemical Structure
  82. GC36000 EPZ020411 hydrochloride EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer. EPZ020411 hydrochloride Chemical Structure
  83. GC16224 EPZ031686 A SMYD3 inhibitor EPZ031686 Chemical Structure
  84. GC12932 EPZ5676 A highly potent DOT1L inhibitor EPZ5676 Chemical Structure
  85. GC65980 EZH2-IN-13 EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity. EZH2-IN-13 Chemical Structure
  86. GC19149 EZM 2302 EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM. EZM 2302 Chemical Structure
  87. GC64900 EZM0414 EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma. EZM0414 Chemical Structure
  88. GC63545 FTX-6058 FTX-6058 ((S)-FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 Chemical Structure
  89. GC63546 FTX-6058 hydrochloride (S)-Pociredir ((S)-FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride Chemical Structure
  90. GC43715 Furamidine (hydrochloride) Furamidine (hydrochloride) (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine (hydrochloride) Chemical Structure
  91. GC38062 Gambogenic acid Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid Chemical Structure
  92. GC36168 GNA002 GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes. GNA002 Chemical Structure
  93. GC50697 GSK 591 dihydrochloride GSK 591 dihydrochloride Chemical Structure
  94. GC15783 GSK126

    A selective EZH2 inhibitor

     GSK126 Chemical Structure
  95. GC19181 GSK2807 Trifluoroacetate GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM. GSK2807 Trifluoroacetate Chemical Structure
  96. GC32693 GSK3326595 (EPZ015938) GSK3326595 (EPZ015938) (EPZ015938) is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM. GSK3326595 (EPZ015938) Chemical Structure
  97. GC36191 GSK3368715 GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. GSK3368715 Chemical Structure
  98. GC49398 GSK3368715 (hydrochloride) An inhibitor of type I PRMTs GSK3368715 (hydrochloride) Chemical Structure
  99. GC36192 GSK3368715 dihydrochloride GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. GSK3368715 dihydrochloride Chemical Structure
  100. GC17534 GSK343 A selective, cell-permeable EZH2 inhibitor GSK343 Chemical Structure
  101. GC11414 GSK503 EZH2 inhibitor GSK503 Chemical Structure

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