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Results for "

PRMT1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15890
    C-7280948

    		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-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-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-12759A
    CARM1-IN-1 hydrochloride
    3 Publications Verification

    		 Histone Methyltransferase Cancer
    CARM1-IN-1 hydrochloride is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7.
    CARM1-IN-1 hydrochloride
  • HY-157151
    iPRMT1

    		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-115758
    PRMT1-IN-1

    		Histone Methyltransferase Cancer
    PRMT1-IN-1 is a PRMT1 inhibitor.
    PRMT1-IN-1
  • HY-111030
    PRMT1-IN-2

    		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-P1182
    C21

    		Histone Methyltransferase Cancer
    C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC50 of 1.8 μM. C21 inhibits PRMT6 with an IC50 of 8.8 μM .
    C21
  • HY-164456
    AMI-408

    		Histone Methyltransferase Cancer
    AMI-408 is a PRMT1 inhibitor. AMI-408 can reduce H4R3me2as level in MLL-GAS7 leukemia cells .
    AMI-408
  • HY-110137A
    Furamidine

    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-110137
    Furamidine dihydrochloride
    2 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-162003
    DCPT1061

    		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-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-168142
    YD1130

    		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-19615
    MS023
    10+ Cited Publications

    		 Histone Methyltransferase Cancer
    MS023 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-19615B
    MS023 dihydrochloride
    10+ 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-19615A
    MS023 trihydrochloride

    		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
    PRMT4-IN-2

    		Others 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-12759
    CARM1-IN-1
    3 Publications Verification

    		 Histone Methyltransferase Cancer
    CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
    CARM1-IN-1
  • HY-18962
    AMI-1
    5 Publications Verification

    		 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-100855
    DC_C66

    		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-18962A
    AMI-1 free acid
    5 Publications Verification

    		 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-128717C
    GSK3368715 hydrochloride

    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
    (1-Nitroethene-1,2-diyl)dibenzene

    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-128717
    GSK3368715

    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-128717A
    GSK3368715 dihydrochloride
    Maximum Cited Publications
    14 Publications Verification

    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-128717B
    GSK3368715 trihydrochloride

    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-120137
    CMP-5

    		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-113846
    CMP-5 hydrochloride

    		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-161334
    CARM1-IN-4

    		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-113846A
    CMP-5 dihydrochloride

    		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-107574
    TC-E 5003

    		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

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