Search Site
  • 0
    My Cart

    Click Here to Find How Many Items You Have Added:)

    image loader

    Adding item(s) to cart......

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. GC14585 GSK591 PRMT5 inhibitor GSK591 Chemical Structure
  3. GP10020 Histone-H2A-(107-122)-Ac-OH

    Histone-H2A peptide

     Histone-H2A-(107-122)-Ac-OH Chemical Structure
  4. GC17023 HLCL-61 HLCL-61 is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5). HLCL-61 Chemical Structure
  5. GC19465 JNJ-64619178 JNJ-64619178 is a PRMT5 inhibitor JNJ-64619178 Chemical Structure
  6. GC19211 JQEZ5 JQEZ5 is a novel and potent EZH2 inhibitor. JQEZ5 Chemical Structure
  7. GC33184 LLY-283 A PRMT5 inhibitor LLY-283 Chemical Structure
  8. GC16261 LLY507 SMYD2 inhibitor LLY507 Chemical Structure
  9. GC63056 MAK683-CH2CH2COOH

    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 and PROTAC EED degrader-2.

     MAK683-CH2CH2COOH Chemical Structure
  10. GC65254 MC4355 MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC). MC4355 Chemical Structure
  11. GC61058 Metoprine Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine Chemical Structure
  12. GC14652 MM-102 MLL1 inhibitor,high-affinity peptidomimetic MM-102 Chemical Structure
  13. GC36632 MM-102 TFA MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki 200 times more potent than the ARA peptide. MM-102 TFA Chemical Structure
  14. GC67758 MM-401 TFA MM-401 TFA Chemical Structure
  15. GC33278 MM-589 MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM. MM-589 Chemical Structure
  16. GC65037 MM-589 TFA MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM. MM-589 TFA Chemical Structure
  17. GC61468 MR837 MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain). MR837 Chemical Structure
  18. GC50576 MRK 740 Potent PRDM9 inhibitor MRK 740 Chemical Structure
  19. GC63558 MRTX-1719 MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells. MRTX-1719 Chemical Structure
  20. GC69499 MRTX-1719 hydrochloride

    MRTX-1719 hydrochloride is an effective, novel, and selective inhibitor of the PRMT5/MTA complex. Its IC50 value for PRMT5/MTA MTAPDEL SDMA cell lines is <10 nM.

     MRTX-1719 hydrochloride Chemical Structure
  21. GC62715 MRTX9768 MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. MRTX9768 Chemical Structure
  22. GC63080 MRTX9768 hydrochloride MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. MRTX9768 hydrochloride Chemical Structure
  23. GC10099 MS023

    MS023 is a potent, selective, and cell-active inhibitor of type I protein arginine methyltransferases (PRMTs).

     MS023 Chemical Structure
  24. GC16432 MS023 (hydrochloride) type I PRMTs inhibitor MS023 (hydrochloride) Chemical Structure
  25. GC36655 MS023 dihydrochloride MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively. MS023 dihydrochloride Chemical Structure
  26. GC36656 MS049 MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells. MS049 Chemical Structure
  27. GC14240 MS049 (hydrochloride) MS049 (hydrochloride) is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 (hydrochloride) reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 (hydrochloride) is not toxic and does not affect the growth of HEK293 cells. MS049 (hydrochloride) Chemical Structure
  28. GC64295 MS67 MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects. MS67 Chemical Structure
  29. GC69504 MS8815

    MS8815 is a selective PROTAC degrader of zeste homolog 2 (EZH2). It has inhibitory activity against EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for research on triple-negative breast cancer (TNBC).

     MS8815 Chemical Structure
  30. GC61142 NSC745885 NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple?cancer?cell lines but not normal cells.?NSC745885 is an effective?down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced?bladder?and oral squamous cell carcinoma (OSCC) cancers. NSC745885 Chemical Structure
  31. GC64772 NV03 NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity. NV03 Chemical Structure
  32. GC16397 OICR-9429 Wdr5-MLL interaction antagonist OICR-9429 Chemical Structure
  33. GC69636 OTS193320

    OTS193320 is an imidazopyridine compound, a SUV39H2 methyltransferase activity inhibitor. OTS193320 reduces the global histone H3 lysine 9 trimethylation level in breast cancer cells and induces apoptosis cell death. Compared to single-agent OTS193320 or DOX, the combination of OTS193320 with Doxorubicin (DOX; A) can lead to a decrease in γ-H2AX levels and cancer cell viability.

     OTS193320 Chemical Structure
  34. GC50367 PF 06726304 acetate Highly potent and SAM-competitive EZH2 inhibitor PF 06726304 acetate Chemical Structure
  35. GC32977 PF-06726304 PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity. PF-06726304 Chemical Structure
  36. GC17956 PFI-2 SETD7 methyltransferase inhibitor PFI-2 Chemical Structure
  37. GC12530 PFI-2 (hydrochloride) PFI-2 (hydrochloride) Chemical Structure
  38. GC64941 PR5-LL-CM01 PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies. PR5-LL-CM01 Chemical Structure
  39. GC36969 PRMT5-IN-1 PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions. PRMT5-IN-1 Chemical Structure
  40. GC65027 PRMT5-IN-20 PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity. PRMT5-IN-20 Chemical Structure
  41. GC62187 PROTAC EED degrader-1 PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit. PROTAC EED degrader-1 Chemical Structure
  42. GC62717 PROTAC EED degrader-2 PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit. PROTAC EED degrader-2 Chemical Structure
  43. GC65509 PROTAC EZH2 Degrader-1 PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes. PROTAC EZH2 Degrader-1 Chemical Structure
  44. GC46213 Ro 41-0960 A COMT inhibitor Ro 41-0960 Chemical Structure
  45. GC18650 S-(5'-Adenosyl)-L-methionine (tosylate) S-(5'-Adenosyl)-L-methionine (SAM) is a ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by DNA and protein methyltransferases. S-(5'-Adenosyl)-L-methionine (tosylate) Chemical Structure
  46. GC44859 S-(5'-Adenosyl)-L-methionine chloride (hydrochloride) S-(5'-Adenosyl)-L-methionine chloride (SAM) is a ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by DNA and protein methyltransferases. S-(5'-Adenosyl)-L-methionine chloride (hydrochloride) Chemical Structure
  47. GC44886 S-Farnesyl Thioacetic Acid S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine which behaves as a competitive inhibitor of isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). S-Farnesyl Thioacetic Acid Chemical Structure
  48. GC62555 SETD2-IN-1 TFA SETD2-IN-1 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. SETD2-IN-1 TFA has anti-proliferative effects. SETD2-IN-1 TFA Chemical Structure
  49. GC64893 SETDB1-TTD-IN-1 SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD. SETDB1-TTD-IN-1 Chemical Structure
  50. GC64894 SETDB1-TTD-IN-1 TFA SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD. SETDB1-TTD-IN-1 TFA Chemical Structure
  51. GC11491 SGC 0946 A potent inhibitor of DOT1L SGC 0946 Chemical Structure
  52. GC50699 SGC 6870 SGC 6870 Chemical Structure
  53. GC19329 SGC2085 SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM. SGC2085 Chemical Structure
  54. GC18428 SGC2085 (hydrochloride) SGC2085 is an inhibitor of protein arginine methyltransferase 4 (PRMT4/CARM1; IC50 = 50 nM). SGC2085 (hydrochloride) Chemical Structure
  55. GC12874 SGC707 PRMT3 inhibitor SGC707 Chemical Structure
  56. GC14364 SGI-1027 DNMT inhibitor SGI-1027 Chemical Structure
  57. GC34784 Sinefungin A methyltransferase inhibitor Sinefungin Chemical Structure
  58. GC37654 SMYD3-IN-1 SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM. SMYD3-IN-1 Chemical Structure
  59. GC18642 SW155246 SW155246 is an inhibitor of DNA methyltransferase 1 (DNMT1; IC50 = 1.2 μM). SW155246 Chemical Structure
  60. GC62390 SW2_110A SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro. SW2_110A Chemical Structure
  61. GC69980 SW2_152F

    SW2_152F is an effective selective inhibitor of chromobox 2 chromodomain (CBX2 ChD), with a Kd of 80 nM. In vitro, SW2_152F exhibits selectivity for CBX2 ChD that is 24-1000 times higher than other CBX paralogs.

     SW2_152F Chemical Structure
  62. GC67676 Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH Chemical Structure
  63. GC38163 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat hydrobromide Chemical Structure
  64. GC17672 TC-E 5003 PRMT1 inhibitor, potent TC-E 5003 Chemical Structure
  65. GC70041 TNG908

    TNG908 is a blood-brain barrier penetrable MTAP-cooperative PRMT5 inhibitor. TNG908 has 15 times higher selectivity for MTAPnull cell lines than for MTAPWT cell lines and can be used in cancer research.

     TNG908 Chemical Structure
  66. GC45763 Tolcapone-d4 An internal standard for the quantification of tolcapone Tolcapone-d4 Chemical Structure
  67. GC41263 TP-064 TP-064 is a potent inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 in vitro. TP-064 Chemical Structure
  68. GC15688 UNC 0224 A potent inhibitor of G9a histone methyltransferase UNC 0224 Chemical Structure
  69. GC12548 UNC 0631 G9a inhibitor UNC 0631 Chemical Structure
  70. GC14249 UNC 0642 G9a and GLP histone lysine methyltransferase inhibitor UNC 0642 Chemical Structure
  71. GC16518 UNC 0646 An inhibitor of G9a/GLP methyltransferases UNC 0646 Chemical Structure
  72. GC50082 UNC 2399 UNC 2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM. UNC 2399 Chemical Structure
  73. GC15652 UNC 2400 negative control of UNC1999 UNC 2400 Chemical Structure
  74. GC37856 UNC0321 UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E. UNC0321 Chemical Structure
  75. GC16741 UNC0379 N-lysine methyltransferase SETD8 inhibitor UNC0379 Chemical Structure
  76. GC34160 UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) Chemical Structure
  77. GC15610 UNC0638 A G9a and GLP histone methyltransferase inhibitor UNC0638 Chemical Structure
  78. GC16794 UNC1215 Potent L3MBTL3 domain inhibitor UNC1215 Chemical Structure
  79. GC11375 UNC1999

    EZH2 inhibitor

     UNC1999 Chemical Structure
  80. GC45117 UNC2327 An allosteric inhibitor of PRMT3 UNC2327 Chemical Structure
  81. GC17207 UNC3866 a potent antagonist of CBX4 and CBX7 chromodomains UNC3866 Chemical Structure
  82. GC70091 UNC4976 TFA

    UNC4976 TFA is a positive allosteric modulator (PAM) peptide that binds to the chromodomain and nucleic acid binding domain of CBX7. UNC4976 TFA antagonizes the specific recruitment of CBX7 to target genes by H3K27me3, while increasing non-specific binding to DNA and RNA.

     UNC4976 TFA Chemical Structure
  83. GC18096 UNC669 L3MBTL antagonist,potent and selective UNC669 Chemical Structure
  84. GC64083 UNC6934 UNC6934, a chemical probe targeting the PWWP domain, alters NSD2 nucleolar localization. UNC6934 Chemical Structure
  85. GC33397 Valemetostat A dual EZH1 and EZH2 inhibitor Valemetostat Chemical Structure
  86. GC37881 Valemetostat tosylate Valemetostat tosylate (DS-3201 tosylate), a first-in-class EZH1/2 dual inhibitor. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma. Valemetostat tosylate Chemical Structure
  87. GC14763 WDR5 0103 WD repeat-containing protein 5 (WDR5) antagonist WDR5 0103 Chemical Structure
  88. GC62558 WDR5-IN-1 WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines. WDR5-IN-1 Chemical Structure
  89. GC19388 XY1 XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive. XY1 Chemical Structure
  90. GC45609 ZLD1039 An inhibitor of EZH2 ZLD1039 Chemical Structure

Items 101 to 189 of 189 total

per page
  2. 1
  3. 2

Set Descending Direction