Histone Methyltransferase

VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.

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

MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.

SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias.

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

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.

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 MTAP DEL SDMA cells.

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

SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.

Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor.

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

(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.

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.

CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.

(R)-HH2853 is a potent EZH2 inhibitor with an IC50 <100 nM for EZH2-Y641F.(R)-HH2853 has anticancer and antitumor activity and can be used in autoimmune diseases.

(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.

MS0124 is a potent and selective G9A-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM, respectively.

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.

WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.

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.

MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .

UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.

PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.

CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.

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.

ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

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

CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

DW14800 is an inhibitor of PRMT5 (IC50 = 17 nM), enhances the transcription of HNF4α, and reduces the level of H4R3me2s.

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

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

Menin-MLL inhibitor MI-2 (MI2) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.

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.

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

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

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

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

MS023 trihydrochloride (MS023 3HCl) is a selective and potent human type I protein arginine methyltransferase (PRMT) inhibitor with potential anticancer activity against PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8 for cancer research.

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

BML-278 is a SIRT1 activator with an EC150 of 1 μM.BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in parental and maternal prokaryotes, and can be used to improve early embryonic development.BML-278 induces cell cycle arrest in primary human mesenchymal stromal cells at the G1/S phase, and can be used to delay senescence.BML-278 reduces microtubule protein acetylation in U937 cells and increases mitochondrial density in mouse C2C12 myoblasts. BML-278 reduces microtubule protein acetylation in U937 cells and increases mitochondrial density in mouse C2C12 myoblasts.

Anticancer agent 126 (compound 12), a WDR5 inhibitor, exhibits anticancer properties by disrupting the WDR5-MYC interaction in cells, subsequently reducing MYC target gene expression [1].

CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485

NSD2-IN-4 is a potent, selective inhibitor of the NSD2-SET domain, showing promise for the treatment of diseases related to NSD2 [1].

MS9715 is a potent and selective NSD3-targeting PROTAC, designed by leveraging BI-9321, which targets the PWWP1 domain of NSD3, in conjunction with an E3 ligase VHL ligand. This compound holds potential for research in NSD3-dependent cancer treatments [1].