Histone Methyltransferase

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.

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.

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.

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]

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.

PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.

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.

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

EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.

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.

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.

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.

Tulmimetostat (CPI-0209) is an orally active EZH1 EZH2 inhibitor with antitumor activity, utilized in the study of ovarian cancer and advanced solid tumors.

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].

(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.

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.

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.

Lem-14-1189, a LEM-14 derivative, is a potent NSD inhibitor of the nuclear receptor binding SET domain, and has inhibitory effects on NSD1, NSD2, and NSD3, with IC50 of 418 μM, 111 μM, and 60 μM, respectively. LEM-14-1189 has potential anticancer activity and can be used to study multiple myeloma (MM) and diseases of the blood system.

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.

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.

TNG908 is an orally active and selective MTAP-co-PRMT5 inhibitor that crosses the blood-brain barrier and kills MTAP-deficient cancers.

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.

Ziftomenib (KO-539) is an inhibitor of menin-MLL interaction with antitumor activity, suitable for leukemia research.

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.

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.

GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).

UNC0642 is an effective and specific G9a GLP inhibitor (IC50< 2.5 nM).

SGC707 is a potent, selective, and cell-active allosteric inhibitor of [PRMT3].

AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).

GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).

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

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.

EBI-2511 is a highly potent, orally active inhibitor of EZH2, with an IC50 of 6 nM in Pfeffiera cell lines.

EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

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.

EPZ004777 is a potent and selective DOT1L inhibitor with an IC50 of 0.4 nM.

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.

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity.

MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Valemetostat (DS-3201) is an EZH1 2 inhibitor that can be used to study relapsed refractory peripheral T-cell lymphoma.

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.

AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.

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.

MIV-6R inhibits Menin-MLL interaction (IC50: 56 nM) and can be used to study leukemia.