histone methyltransferase

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.

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

3-Deazaneplanocin A HCl is a synthetically derived inhibitor of the histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (SAHH). By regulating epigenetic methylation pathways, 3-deazaneplanocin A induces apoptosis and inhibits tumor cell proliferation, demonstrating significant antitumor activity in various tumor models. 3-deazaneplanocin A HCl can be used in research on epigenetic regulation, tumorigenesis and progression, and stem cell differentiation.

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.

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.

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.

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.

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

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

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

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.

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.

Sinefungin (Adenosyl-Ornithine) belongs to natural products and is an mRNA methyltransferase inhibitor with broad-spectrum antiviral activity. This compound possesses cell permeability and is commonly used in antiviral mechanism research and antiviral drug development.

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).

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

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

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.

(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.

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

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 .

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.

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.

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.