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.

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 and selective inhibitor of the PRMT5 MTA complex with an IC50 value of <10 nM against PRMT5 MTAMTAPDELSDMA cell lines.

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.

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.

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

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.

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.

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.

(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.

(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.

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.

AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

(2R,4S)-Azalanstat (Iso-Azalansta) is a selective heme oxygenase (HO) inhibitor that is used in the study of cardiovascular disease.

lutidinic acid (2,4-Dicarboxypyridine) is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases.

EZH2-IN-13, a potent EZH2 inhibitor, exhibits potential anticancer activity and may be utilized to study diseases associated with EZH2 activity.

Cyproheptadine hydrochloride sesquihydrate (Peritol), an antihistamine, is an antagonist of serotonin and histamine2.

GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM).

SGC-iMLLT is a potent and selective MLLT1 3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target engagement of MLLT1(Kd = 0.129 μM) and MLLT3(Kd = 0.077 μM).