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PRMT1 inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19615
    MS023
    Maximum Cited Publications
    22 Publications Verification

    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-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-12970A
    EPZ020411 hydrochloride
    5+ Cited Publications

    Histone Methyltransferase Apoptosis Cancer
    EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer .
    EPZ020411 hydrochloride
  • 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-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-12970
    EPZ020411
    5+ Cited Publications

    Histone Methyltransferase Apoptosis Cancer
    EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer .
    EPZ020411
  • 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-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-15890

    Histone Methyltransferase Cancer
    C-7280948 is a selective and potent protein methyltransferase1 (PRMT1) inhibitor with an IC50 value of 12.75 μM .
    C-7280948
  • HY-19615B
    MS023 dihydrochloride
    Maximum Cited Publications
    22 Publications Verification

    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-138993A

    Amine N-methyltransferase Cancer
    NNMT-IN-6 hydrochloride is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 hydrochloride inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 hydrochloride can be used for the research of oral cancer .
    NNMT-IN-6 hydrochloride
  • 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-12759
    CARM1-IN-1
    4 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1
  • HY-12759A
    CARM1-IN-1 hydrochloride
    4 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1 hydrochloride
  • HY-138993

    Amine N-methyltransferase Cancer
    NNMT-IN-6 is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 can be used for the research of oral cancer .
    NNMT-IN-6
  • 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-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-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-120137

    Histone Methyltransferase Cancer
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected .
    CMP-5
  • HY-157151

    Histone Methyltransferase Cancer
    iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
    iPRMT1
  • HY-178446

    METTL3 c-Myc Bcl-2 Family Cancer
    METTL3-IN-11 is an excellent, selective METTL3 inhibitor (IC50 = 45.31 nM). METTL3-IN-11 exhibits high selectivity towards METTL3 compared to DNMT1, EZH1, MLL1, and PRMT1. METTL3-IN-11 reduces the m6A level of total RNA in MOLM-13 and SKOV3 cells, induces cell apoptosis, and inhibits cell migration. METTL3-IN-11 can reduce the expression of m6A downstream target genes (c-MYC and BCL2). METTL3-IN-11 can be used for the study of ovarian cancer and acute myeloid leukemia .
    METTL3-IN-11
  • HY-164456

    Histone Methyltransferase Cancer
    AMI-408 is a PRMT1 inhibitor. AMI-408 can reduce H4R3me2as level in MLL-GAS7 leukemia cells .
    AMI-408
  • HY-161334

    Histone Methyltransferase Apoptosis Cancer
    CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
    CARM1-IN-4
  • HY-115758

    Histone Methyltransferase Cancer
    PRMT1-IN-1 is a PRMT1 inhibitor.
    PRMT1-IN-1
  • HY-178114

    Histone Methyltransferase Apoptosis Cancer
    SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer .
    SKLB-0124
  • 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-162003

    Histone Methyltransferase Cancer
    DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 has antitumor effect .
    DCPT1061
  • HY-110137R

    DB75 dihydrochloride (Standard); NSC 305831 dihydrochloride (Standard)

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Reference Standards Infection Inflammation/Immunology Cancer
    Furamidine (dihydrochloride) (Standard) is the analytical standard of Furamidine (dihydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-168142

    Histone Methyltransferase Cancer
    YD1130 is a PRMT4 inhibitor (0.5 nM, 75% inhibition rate), and its inhibitory potency against other PRMTs is not significant (PRMT5 IC50> 1 μM, PRMT1/3/6/7/8 IC50 > 10 μM). .
    YD1130
  • HY-19615A

    Histone Methyltransferase Cancer
    MS023 trihydrochloride 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 trihydrochloride
  • HY-155154

    Histone Methyltransferase Cancer
    PRMT4-IN-2 (compound 55) is a pan-inhibitor of protein arginine methyltransferase (PRMT) with IC50s of 92 nM (PRMT4), 436 nM (PRMT6), 460 nM (PRMT1), 823 nM ( PRMT8), 1.386 μM (PRMT3) .
    PRMT4-IN-2
  • HY-100855

    Histone Methyltransferase Cancer
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5 .
    DC_C66
  • 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-W013500

    alpha-Nitrostilbene; α-Nitrostilbene; NSC 385

    Histone Methyltransferase Others
    (1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
    (1-Nitroethene-1,2-diyl)dibenzene
  • HY-128717B

    EPZ019997 trihydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 trihydrochloride (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 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
    GSK3368715 trihydrochloride
  • HY-18962R

    Histone Methyltransferase Cancer
    AMI-1 (Standard) is the analytical standard of AMI-1. This product is intended for research and analytical applications. 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 (Standard)
  • HY-113846A

    Histone Methyltransferase Cancer
    CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected .
    CMP-5 dihydrochloride
  • HY-113846

    Histone Methyltransferase Cancer
    CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected .
    CMP-5 hydrochloride
  • HY-18962AR

    Histone Methyltransferase Cancer
    AMI-1 (free acid) (Standard) is the analytical standard of AMI-1 (free acid). This product is intended for research and analytical applications. 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 (Standard)
  • HY-182297

    Histone Methyltransferase Ligands for Target Protein for PROTAC Cancer
    PRMT1 ligand-1 is a PRMT1 ligand. PRMT1 ligand-1 can be used as a target protein ligand to develop and design degraders of PROTAC PRMT1, such as PROTAC PRMT1 degrader-1 (HY-182275). PROTAC PRMT1 degrader-1 inhibits the growth of various cancer cells .
    PRMT1 ligand-1
  • HY-182275

    PROTACs Histone Methyltransferase Cancer
    PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
    PROTAC PRMT1 degrader-1
  • HY-186045

    Histone Methyltransferase Apoptosis DNA/RNA Synthesis ATP-binding cassette (ABC) transporters Cancer
    SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC) .
    SKLB06489
  • HY-114510

    Discoidin Domain Receptor Histone Acetyltransferase Sirtuin Fungal Apoptosis Infection Cancer
    PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
    PRMT/HKMT-IN-1
  • HY-107574R

    Reference Standards Histone Methyltransferase AP-1 NF-κB PKA Metabolic Disease Inflammation/Immunology Cancer
    TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. 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 (Standard)

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