Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
125 Results for "
protein methyltransferases
" in MedChemExpress (MCE) Product Catalog:
Products (125)
125 Results for "protein methyltransferases" in MCE Product Catalog:
34
34 Publications Verification
Synonyms: GSK3326595; EPZ015938
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
24
24 Cited Publications
Cat. No.: HY-19615
CAS No.: 1831110-54-3
Target:
Research Areas:
MS023, a chemical probe, is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .
24
24 Cited Publications
Cat. No.: HY-19615B
CAS No.: 1992047-64-9
Target:
Research Areas:
MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .
21
21 Cited Publications
Synonyms: EPZ019997 dihydrochloride
Target:
Research Areas:
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
21
Target:
Research Areas:
GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
15
15 Cited Publications
Synonyms: EPZ015866; GSK3203591
Target:
Research Areas:
GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
12
12 Cited Publications
Synonyms: JNJ-64619178
Target:
Research Areas:
Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer .
12
12 Cited Publications
Cat. No.: HY-19715
CAS No.: 1687736-54-4
Target:
Research Areas:
SGC707, a chemical probe, is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC50=31 nM, Kd=53 nM).
11
11 Cited Publications
Cat. No.: HY-19313
CAS No.: 1793053-37-8
Target:
Research Areas:
LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes .
7
7 Cited Publications
Target:
Research Areas:
LLY-283, a chemical probe, is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity .
7
7 Cited Publications
Cat. No.: HY-18962
CAS No.: 20324-87-2
Target:
Research Areas:
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
7
Target:
Research Areas:
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
6
6 Cited Publications
Target:
Research Areas:
EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
6
6 Cited Publications
Target:
Research Areas:
SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
6
6 Cited Publications
Cat. No.: HY-141539A
Purity: 99.77%
Target:
Research Areas:
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
4
4 Cited Publications
Target:
Research Areas:
TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers .
4
4 Cited Publications
Target:
Research Areas:
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
4
4 Cited Publications
Cat. No.: HY-122181B
Purity: 99.58%
Target:
Research Areas:
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
4
4 Cited Publications
Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride
Research Areas:
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
4
4 Cited Publications
Synonyms: HMTase Inhibitor IX
Research Areas:
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
