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Histone Methyltransferase

Histone methyltransferases (HMT) are histone-modifying enzymes , that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. The attachment of methyl groups occurs predominantly at specific lysine or arginine residues on histones H3 and H4.

MRTX-1719
T402542630904-45-7
MRTX-1719 is a potent and selective inhibitor of the PRMT5 MTA complex with an IC50 value of <10 nM against PRMT5 MTAMTAPDELSDMA cell lines.
  • $398
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Tazemetostat
T17881403254-99-8
Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma follicular lymphoma.
  • $59
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Sinefungin
T1688658944-73-3In house
Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7 9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.
  • $129
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MAK-683 hydrochloride
T96812170606-94-5In house
MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.
  • $195
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SETDB1-TTD-IN-1
T97422755823-12-0In house
SETDB1-TTD-IN-1 is a potent and selective inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD, Kd = 88 nM), and also an endogenous binder competitive inhibitor with a KD of 0.106±0.002 μM for TTD. It can be used to study the biological functions and disease associations of SETDB1-TTD.
  • $269
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EZM 2302
T56051628830-21-6
EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]
  • $68
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PF-06821497
T124301844849-10-0
PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
  • $97
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GSK126
T20791346574-57-9
GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
  • $37
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SNDX-5613
T129432169919-21-3
Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.
  • $67
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EPZ031686
TQ02631808011-22-4
EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.
  • $113
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JNJ-64619178
T156242086772-26-9
JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.
  • $148
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OICR-9429
T69161801787-56-3
OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.
  • $31
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WM-3835
T91022229025-70-9
WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
  • $31
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VTP50469
T133362169916-18-9
VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.
  • $176
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GSK343
T60591346704-33-3
GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.
  • $54
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(Iso)-MS4322
T402332601727-80-2In house
(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.
  • $489 TargetMol
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EZM0414
T99692411748-50-8
EZM0414 is a potent and selective, orally bioavailable inhibitor of SETD2 with an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays, potentially useful for researching relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma [1].
  • $279
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EZH2-IN-15
T678832098545-98-1
EZH2-IN-15 (SHR2554) is a specific inhibitor of the zeste 2 histone modification enhancer (EZH2).EZH2 is aberrantly overexpressed in many human cancers and controls adaptive responses by regulating Treg activity. EZH2 expression in tumors has also been shown to control innate immunity.
  • $159
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TNG908
T734942760481-53-4
TNG908 is an orally active and selective MTAP-co-PRMT5 inhibitor that crosses the blood-brain barrier and kills MTAP-deficient cancers.
  • $333
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OTS186935 FA
T12344L1 In house
OTS186935 FA is a protein methyltransferase SUV39H2 inhibitor.OTS186935 FA inhibits tumor growth in MDA-MB-231 breast cancer cells and A549 lung cancer cells.
  • $98
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GSK3368715 dihydrochloride
T11500L1628925-77-8
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.
  • $56
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Ziftomenib
T395852134675-36-6
Ziftomenib (KO-539) is an inhibitor of menin-MLL interaction with antitumor activity, suitable for leukemia research.
  • $318
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SGC0946
T30821561178-17-3
SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
  • $41
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GSK467
T54841628332-52-4
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
  • $74
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3-deazaneplanocin A HCl
T6360120964-45-6
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
  • $87
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Pinometostat
T30991380288-87-8
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor (Ki=80 pM). Pinometostat has antitumor activity and can be used in experiments to study a variety of leukemia treatments.
  • $34
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UNC0642
T41661481677-78-4
UNC0642 is an effective and specific G9a GLP inhibitor (IC50< 2.5 nM).
  • $34
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AZ505
TQ01001035227-43-0
AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).
  • $58
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SGC707
T30841687736-54-4
SGC707 is a potent, selective, and cell-active allosteric inhibitor of [PRMT3].
  • $59
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EBI-2511
T151942098546-05-3
EBI-2511 is a highly potent, orally active inhibitor of EZH2, with an IC50 of 6 nM in Pfeffiera cell lines.
  • $60
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EPZ004777
T30811338466-77-5
EPZ004777 is a potent and selective DOT1L inhibitor with an IC50 of 0.4 nM.
  • $33
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EPZ015666
T60761616391-65-1
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
  • $42
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Amodiaquine
T838186-42-0
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
  • $44
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MAK683
T152011951408-58-4In house
MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).
  • $48
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M‑89
T119252363165-42-6
M-89, a highly potent and specific inhibitor of the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction, exhibits a Kd of 1.4 nM for menin binding. This compound holds potential for treating MLL leukemia.
  • $169
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Valemetostat
T13279L1809336-39-7
Valemetostat (DS-3201) is an EZH1 2 inhibitor that can be used to study relapsed refractory peripheral T-cell lymphoma.
  • $96
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Tulmimetostat
T401992567686-02-4
Tulmimetostat (CPI-0209) is an orally active EZH1 EZH2 inhibitor with antitumor activity, utilized in the study of ovarian cancer and advanced solid tumors.
  • $30
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UNC 0631
T23541320288-19-4
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
  • $42
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BIX-01294
T7697935693-62-2
BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
  • $34
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GSK3326595
T57451616392-22-3In house
GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
  • $39
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BI-9321 trihydrochloride
T10538L2387510-87-2In house
BI-9321 trihydrochloride (BI9321 trihydrochloride) is a selective and potent NSD3-PWWP1 antagonist that downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells.
  • $45
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AMG-193
T856452790567-82-5
AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.
  • $195
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EPZ032597
T700871887193-58-9In house
EPZ032597 is a novel selective inhibitor of SMYD2 with an IC50 of 16 nM. EPZ032597 has anticancer activity and can be used to prevent and treat pancreatic cancer.
  • $350
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MIV-6R
T244721560968-55-9In house
MIV-6R inhibits Menin-MLL interaction (IC50: 56 nM) and can be used to study leukemia.
  • $293
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TP-064
T289962080306-20-1
TP-064 is a potent and selective PRMT4 inhibitor, featuring an IC50 < 10nM for methylation of H3 (1-25) and over 100-fold selectivity compared to other histone methyltransferases and non-epigenetic targets. It inhibits the methylation of MED12 in cells with an IC50 of 43 nM.
  • $32
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MM-102
T63331417329-24-8
MM-102 (HMTase Inhibitor IX) is a potent inhibitor of WDR5 MLL interaction with IC50 of 2.4 nM and Ki of less than 1 nM in a WDR5 binding assay. MM-102 can also specifically inhibit cell growth and induce apoptosis in leukemia cells carrying MLL1 fusion protein.
  • $33
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UNC0638
T32571255580-76-7
UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
  • $54
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UNC6852
T139542688842-08-0
UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
  • $135
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