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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. GC70906 (R)-HH2853 (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 Chemical Structure
  4. GC11340 (R)-PFI 2 hydrochloride

    (-)PFI2

     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
  5. 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
  6. GC13634 (S)-PFI-2 (hydrochloride)

    (+)-PFI-2

     Negative control of (R)-PFI 2 hydrochloride (S)-PFI-2 (hydrochloride) Chemical Structure
  7. GC17907 3-Deazaneplanocin A (DZNep) hydrochloride

    2,3DMMC

     3-Deazaneplanocin A (DZNep) hydrochloride is an adenosine analogue and is a competitive S-adenosylhomocysteine hydrolase inhibitor with a Ki of 50 pM in cell-free tests. 3-Deazaneplanocin A (DZNep) hydrochloride Chemical Structure
  8. GC13145 3-Deazaneplanocin,DZNep

    DZNep, NSC 617989

    An inhibitor of lysine methyltransferase EZH2

     3-Deazaneplanocin,DZNep Chemical Structure
  9. GC16015 A 366 G9a/GLP histone lysine methyltransferase inhibitor A 366 Chemical Structure
  10. GC32861 A-196 A selective inhibitor of SUV420H1 and SUV420H2 A-196 Chemical Structure
  11. 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
  12. GC30503 A-893 A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM. A-893 Chemical Structure
  13. GC73923 AC1Q3QWB

    AQB

     AC1Q3QWB upregulates CDKN1A and SOX17 by interrupting the HOTAIR-EZH2 interaction and enhances the efficacy of Tazemetostat in endometrial cancer. AC1Q3QWB Chemical Structure
  14. 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
  15. GC17275 AMI-1 A cell permeable inhibitor of PRMTs AMI-1 Chemical Structure
  16. GC42784 AMI-1 (sodium salt)

    Arginine N-Methyltransferase Inhibitor-1

     Protein arginine methyltransferases (PRMTs) post-translationally modify proteins, including histones, and in this way regulate gene expression, signal transduction, and protein-protein interactions. AMI-1 (sodium salt) Chemical Structure
  17. 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
  18. GC17546 AMI5 Eosin Y (disodium) is a soluble acid red dye molecule. AMI5 Chemical Structure
  19. GC42790 Amodiaquine

    Camoquine, Flavoquine, NSC 13453, SN 10751

     Amodiaquine is an aminoquinoline antimalarial compound. Amodiaquine Chemical Structure
  20. 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
  21. GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor Amodiaquine dihydrochloride dihydrate Chemical Structure
  22. GC73278 Anticancer agent 126 Anticancer agent 126 (compound 12) is a WDR5 inhibitor with anticancer effects. Anticancer agent 126 Chemical Structure
  23. 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
  24. 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
  25. 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
  26. GC13744 AZ505 SMYD2 inhibitor,potent and selective AZ505 Chemical Structure
  27. GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor AZ505 ditrifluoroacetate Chemical Structure
  28. 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
  29. GC18159 BAY-598

    A potent and selective SMYD2 inhibitor

     BAY-598 Chemical Structure
  30. GC45389 BAY-6035   BAY-6035 Chemical Structure
  31. GC18161 BCI-121

    A substrate-competitive SMYD3 inhibitor?

     BCI-121 Chemical Structure
  32. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain BI 9321 Chemical Structure
  33. 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
  34. GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT Bisubstrate Inhibitor 78 Chemical Structure
  35. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase BIX 01294 Chemical Structure
  36. GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) is a histone lysine methyltransferase inhibitor. BIX-01338 hydrate (BIX01338 hydrate) Chemical Structure
  37. 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
  38. GC25159 BMF-219 BMF-219 is a highly selective and irreversible inhibitor of menin which has shown very promising activity in in-vitro and in-vivo preclinical tumour models. BMF-219 Chemical Structure
  39. 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
  40. GC10259 BRD4770

    HMTase Inhibitor VI

     novel G9a(EHMT2) inhibitor BRD4770 Chemical Structure
  41. GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays BRD9539 Chemical Structure
  42. GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor C 21 Chemical Structure
  43. GC12005 C7280948 Novel PRMT1 inhibitor C7280948 Chemical Structure
  44. GC73615 CARM1 degrader-1 hydrochloride CARM1 degrader-1 drochloride is the drochloride salt form of CARM1 degrader-1. CARM1 degrader-1 hydrochloride Chemical Structure
  45. GC34108 CARM1-IN-1

    Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor

     A selective inhibitor of PRMT4/CARM1 CARM1-IN-1 Chemical Structure
  46. 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
  47. GC73386 CARM1-IN-3 CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine metltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively. CARM1-IN-3 Chemical Structure
  48. GC73387 CARM1-IN-3 dihydrochloride CARM1-IN-3 didrochloride (compound 17b) is a potent and selective co-activator associated arginine metltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively. CARM1-IN-3 dihydrochloride Chemical Structure
  49. GC18949 CAY10677

    Icmt Inhibitor 15

     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
  50. GC14936 Chaetocin Chaetocin was reported to be a nonspecific inhibitor of histone methyl transferase (HMT) such as SUV39H1, thereby affecting gene expression. Chaetocin Chemical Structure
  51. GC18577 CID-2818500

    α-Nitrostilbene, NSC 385

     An inhibitor of PRMT1 CID-2818500 Chemical Structure
  52. GC70438 cis-BG47 cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. cis-BG47 Chemical Structure
  53. 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
  54. 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
  55. 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
  56. 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
  57. GC16298 CPI-1205 EZH2 inhibitor CPI-1205 Chemical Structure
  58. GC16599 CPI-169 EZH2 inhibitor CPI-169 Chemical Structure
  59. GC10021 CPI-360 EZH2 inhibitor CPI-360 Chemical Structure
  60. 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
  61. GC43354 Cysmethynil

    Icmt Inhibitor

     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
  62. GC48967 D-Homoserine lactone

    D-HSL

     An enantiomer of L-homoserine lactone D-Homoserine lactone Chemical Structure
  63. 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
  64. 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
  65. GC73966 DCPT1061 DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 Chemical Structure
  66. GC73967 DCPT1061 hydrochloride DCPT1061 drochloride has a strong inhibitory effect on PRMT1, PRMT6, and PRMT8 in vitro, The epigenetic enzymes such as PRMT3, PRMT4 and PRMT5 had little inhibitory effect. DCPT1061 hydrochloride Chemical Structure
  67. 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
  68. GC67863 DDO-2093 dihydrochloride DDO-2093 dihydrochloride Chemical Structure
  69. GC47180 Decitabine-15N4

    5-aza-2’-Deoxycytidine-15N4, DAC-15N4

     A neuropeptide with diverse biological activities Decitabine-15N4 Chemical Structure
  70. 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
  71. GC69002 Dot1L-IN-1 TFA

    Dot1L-IN-1 TFA is a highly efficient and selective Dot1L inhibitor with a Ki of 2 pM and IC50<0.1 nM. Dot1L-IN-1 TFA effectively inhibits H3K79 dimethylation in HeLa cells (IC50=3 nM) as well as the activity of the HoxA9 promoter in Molm-13 cells (IC50=17 nM).

     Dot1L-IN-1 TFA Chemical Structure
  72. 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
  73. GC62613 Dot1L-IN-4

    DOT1-like Inhibitor 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
  74. 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
  75. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7 DS-437 Chemical Structure
  76. 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
  77. GC73945 DYB-03 DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 Chemical Structure
  78. 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
  79. GC19130 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. EED226 Chemical Structure
  80. GC67934 EEDi-5285 EEDi-5285 Chemical Structure
  81. 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
  82. 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
  83. GC14756 EI1 EZH2 inhibitor EI1 Chemical Structure
  84. GC69055 EM127

    EM127 (compound 11c) is a highly selective, high-affinity, and site-specific covalent inhibitor of SMYD3 (KD=13 μM). EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 can effectively and persistently weaken the activity of methyltransferases. EM127 can be used for cancer research, especially in SMYD3-positive tumors.

     EM127 Chemical Structure
  85. GC73592 EML734 EML734 is a potent and selective PRMT7/9 inhibitor with IC50 values of 315 nM and 0.89 μM, respectively. EML734 Chemical Structure
  86. GC17334 Entacapone

    OR-611

     Entacapone is a potent, reversible, peripherally acting and orally active inhibitor of catechol-O-methyltransferase (COMT), which effectively inhibits rat liver total COMT with IC50 and Ki values of 20.1nM and 10.7nM, respectively. Entacapone Chemical Structure
  87. GC47294 Entacapone-d10

    OR-611-d10

     An internal standard for the quantification of entacapone Entacapone-d10 Chemical Structure
  88. GC73993 EPIC-0628 EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. EPIC-0628 Chemical Structure
  89. GC14062 EPZ-6438

    E-7438,Tazemetostat

    EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 with a value of inhibition constant Ki of 2.5 nM.

     EPZ-6438 Chemical Structure
  90. 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
  91. GC13383 EPZ004777 EPZ004777, as a potent epigenetic modulators, can reverse TGF-β1 induced T regulatory cells and may be used to treat diverse immune disorders. EPZ004777 Chemical Structure
  92. GC48980 EPZ004777 (formate) A potent inhibitor of DOT1L EPZ004777 (formate) Chemical Structure
  93. GC15259 EPZ004777 HCl EPZ004777 HCl is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM. EPZ004777 HCl Chemical Structure
  94. GC13878 EPZ005687

    EPZ 005687,EPZ-005687

     A potent, selective inhibitor of EZH2 EPZ005687 Chemical Structure
  95. GC19141 EPZ011989 EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase. EPZ011989 Chemical Structure
  96. GC74088 EPZ011989 hydrochloride EPZ011989 drochloride is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor, with a Ki value of <3 nM. EPZ011989 hydrochloride Chemical Structure
  97. GC34136 EPZ011989 trifluoroacetate (EPZ-011989 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
  98. GC15302 EPZ015666

    GSK3235025

     PRMT5 inhibitor EPZ015666 Chemical Structure
  99. GC15102 EPZ020411 PRMT6 inhibitor EPZ020411 Chemical Structure
  100. 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
  101. GC16224 EPZ031686 A SMYD3 inhibitor EPZ031686 Chemical Structure

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