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Results for "

arginine methyltransferase

" in MedChemExpress (MCE) Product Catalog:

72

Inhibitors & Agonists

1

Screening Libraries

2

Peptides

4

Recombinant Proteins

5

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101563
    GSK3326595
    Maximum Cited Publications
    31 Publications Verification

    EPZ015938

    Histone Methyltransferase SARS-CoV MDM-2/p53 CDK Apoptosis Infection Cancer
    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 .
    GSK3326595
  • HY-101564
    Onametostat
    5+ Cited Publications

    JNJ-64619178

    Histone Methyltransferase Cancer
    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 .
    Onametostat
  • HY-19615
    MS023
    20+ Cited Publications

    Histone Methyltransferase Cancer
    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 .
    MS023
  • HY-19715
    SGC707
    10+ Cited Publications

    Histone Methyltransferase Metabolic Disease
    SGC707, a chemical probe, is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC50=31 nM, Kd=53 nM).
    SGC707
  • HY-128717A
    GSK3368715 dihydrochloride
    15+ Cited Publications

    EPZ019997 dihydrochloride

    Histone Methyltransferase Cancer
    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 .
    GSK3368715 dihydrochloride
  • HY-128717
    GSK3368715
    15+ Cited Publications

    EPZ019997

    Histone Methyltransferase Cancer
    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 .
    GSK3368715
  • HY-107777
    LLY-283
    5+ Cited Publications

    Histone Methyltransferase Cancer
    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 .
    LLY-283
  • HY-107574
    TC-E 5003
    3 Publications Verification

    Histone Methyltransferase AP-1 NF-κB PKA Metabolic Disease Inflammation/Immunology Cancer
    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 .
    TC-E 5003
  • HY-18962
    AMI-1
    5+ Cited Publications

    Histone Methyltransferase Cancer
    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 .
    AMI-1
  • HY-110137
    Furamidine dihydrochloride
    3 Publications Verification

    DB75 dihydrochloride; NSC 305831 dihydrochloride

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    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 .
    Furamidine dihydrochloride
  • HY-100565
    SGC2085
    1 Publications Verification

    Histone Methyltransferase Cancer
    SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
    SGC2085
  • HY-100025A
    HLCL-61 hydrochloride
    2 Publications Verification

    Histone Methyltransferase Apoptosis Cancer
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
    HLCL-61 hydrochloride
  • HY-19615B
    MS023 dihydrochloride
    20+ Cited Publications

    Histone Methyltransferase Cancer
    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 .
    MS023 dihydrochloride
  • HY-111213

    Histone Methyltransferase Cancer
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity .
    PRMT5-IN-20
  • HY-109963

    Histone Methyltransferase Cancer
    PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies .
    PR5-LL-CM01
  • HY-133740

    Histone Methyltransferase Cancer
    MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM .
    MS117
  • HY-112165

    Histone Methyltransferase Cancer
    PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3 .
    PRMT5-IN-2
  • HY-122096
    DCLX069
    1 Publications Verification

    Histone Methyltransferase Cancer
    DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects .
    DCLX069
  • HY-124131
    DS-437
    1 Publications Verification

    Histone Methyltransferase Inflammation/Immunology Cancer
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
    DS-437
  • HY-156152A

    PROTACs Histone Methyltransferase Cancer
    CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research .
    CARM1 degrader-1 hydrochloride
  • HY-Q36691

    Histone Methyltransferase Cancer
    PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation .
    PRMT5-IN-30
  • HY-128579

    Histone Methyltransferase Cancer
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity .
    DW14800
  • HY-126256A

    Histone Methyltransferase Cancer
    PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
    PRMT5-IN-1 hydrochloride
  • HY-18962A
    AMI-1 free acid
    5+ Cited Publications

    Histone Methyltransferase Cancer
    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 .
    AMI-1 free acid
  • HY-159728

    PROTACs Histone Methyltransferase Apoptosis Early 2 Factor (E2F) c-Myc Cancer
    PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia .
    PROTAC PRMT3 degrader 1
  • HY-110137A

    DB75; NSC 305831

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
    Furamidine
  • HY-156152

    PROTACs Histone Methyltransferase Cancer
    CARM1 degrader-1 is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer .
    CARM1 degrader-1
  • HY-15214A

    Histone Methyltransferase Cancer
    CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
    CARM1-IN-3 dihydrochloride
  • HY-100565A

    Histone Methyltransferase Cancer
    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
    SGC2085 hydrochloride
  • HY-136809

    Histone Methyltransferase Cancer
    PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.
    PRMT6-IN-2
  • HY-126256

    Histone Methyltransferase Cancer
    PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
    PRMT5-IN-1
  • HY-172769

    Histone Methyltransferase Cancer
    CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers .
    CM112
  • HY-176534

    Histone Methyltransferase Cancer
    PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma .
    PRMT5-IN-52
  • HY-117927

    GSK3536023

    Histone Methyltransferase Cancer
    EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM .
    EPZ0025654
  • HY-176701

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
    PRMT5-MTA-IN-4
  • HY-175821

    Histone Methyltransferase Apoptosis Cancer
    PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC .
    PRMT1-IN-3
  • HY-178378

    Histone Methyltransferase GLP Receptor Reactive Oxygen Species (ROS) Autophagy Apoptosis Cancer
    G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer .
    G9a-IN-4
  • HY-144188

    Histone Methyltransferase Cancer
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
    PRMT5-IN-17
  • HY-144187

    Histone Methyltransferase Cancer
    PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
    PRMT5-IN-16
  • HY-P3822

    Histone Methyltransferase Cancer
    PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
    PRMT5-IN-23
  • HY-110158

    Histone Methyltransferase Cancer
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
    UNC2327
  • HY-141875

    Histone Methyltransferase Cancer
    PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (prmt5).
    PRMT5-IN-13
  • HY-100025

    Histone Methyltransferase Cancer
    HLCL-61 is a first-in-class small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5).
    HLCL-61
  • HY-P2556

    Biochemical Assay Reagents Others
    Histone H3 (21-44), derived from histone H3 21-44 amino acids, is usually used as a substrate (such as protein arginine methyltransferases) for methylation assays .
    Histone H3 (21-44)
  • HY-155154A

    Histone Methyltransferase Cancer
    PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50: 37 nM) and PRMT4 (IC50: 253 nM) .
    PRMT4-IN-3
  • HY-111030

    Histone Methyltransferase Cancer
    PRMT1-IN-2 (RM65) is a potent PRMT1 inhibitor with an IC50 of 55.4 μM. PRMT1-IN-2 shows histone hypomethylation in HepG2 cells .
    PRMT1-IN-2
  • HY-164497

    DNA/RNA Synthesis Histone Methyltransferase Cancer
    NSC 641396 is a ribonucleotide reductase (RNR) inhibitor with an IC50 value of 1.2 μM. NSC 641396 is also a protein arginine N-methyltransferase 9 (PRMT9) inhibitor. NSC 641396 has antitumor activity .
    NSC 641396
  • HY-15214

    Histone Methyltransferase Cancer
    CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
    CARM1-IN-3
  • HY-128717C

    EPZ019997 hydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity .
    GSK3368715 hydrochloride
  • HY-153421

    Histone Methyltransferase Cancer
    PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape .
    PRMT5-IN-28

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