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Chromatin/Epigenetic

DNA Methyltransferase

(45)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(82)

Histone Acetyltransferase

(51)

Histone Demethylase

(96)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

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.

Filter HomeSignaling PathwaysChromatin/EpigeneticHistone Methyltransferase

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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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.

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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.

$172

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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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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.

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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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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.

$222

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GSK126

T20791346574-57-9

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).

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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.

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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.

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ORIC-944

T870732369769-29-7

ORIC-944 is an orally available and selective variant of PRC2 with anticancer activity for prostate cancer research.

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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.

$115

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MU1656

T639552766698-38-6In house

MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L (IC50 = 2 nM), a key epigenetic regulatory protein involved in the development of cancers such as hematologic malignancies, thus MU1656 was able to significantly inhibit the proliferation of cancer cells and induce apoptosis.

$2,390

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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]

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LLY-507

T68791793053-37-8

LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.

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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.

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CM-272

T71941846570-31-7

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

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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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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.

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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.

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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.

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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.

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