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PRMTs

" in MedChemExpress (MCE) Product Catalog:

222

Inhibitors & Agonists

1

Peptides

2

Natural
Products

3

Isotope-Labeled Compounds

26

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-139611
    Navlimetostat
    3 Publications Verification

    MRTX-1719; BMS-986504

    Histone Methyltransferase Cancer
    Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
    Navlimetostat
  • 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-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-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-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-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-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-173561

    PROTACs Histone Methyltransferase Cancer
    MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer .
    MS115
  • HY-151576

    Histone Methyltransferase Cancer
    PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
    PRMT5:MEP50 PPI
  • HY-139611C
    Navlimetostat hydrochloride
    3 Publications Verification

    MRTX-1719 hydrochloride; BMS-986504 hydrochloride

    Histone Methyltransferase Cancer
    Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
    Navlimetostat hydrochloride
  • HY-173557

    Histone Methyltransferase Apoptosis Cancer
    PRMT7-IN-2 (A33) is a selective PRMT7 inhibitor with an IC50 of 0.50 μM. PRMT7-IN-2 arrests cell cycle at G0/G1 phase, induces cell apoptosis, and inhibits cell growth in vivo and in vitro. PRMT7-IN-2 decreases the monomethylarginine level of PRMT7, increases expression of epithelial marker (E-cadherin, and reduces expression of mesenchymal markers such as N-cadherin, Vimentin, and ZEB2 .
    PRMT7-IN-2
  • 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-132309
    BRD0639
    1 Publications Verification

    Histone Methyltransferase Cancer
    BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
    BRD0639
  • 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-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-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-W280124

    Histone Methyltransferase Cancer
    PRMT9-IN-1 is a PRMT9 inhibitor. PRMT9-IN-1 can be used in the research of hematological cancer .
    PRMT9-IN-1
  • 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-147185

    Histone Methyltransferase Cancer
    PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells .
    PRMT7-IN-1
  • HY-160865

    Histone Methyltransferase Cancer
    PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM. PRMT5-IN-35 can be used in cancer research .
    PRMT5-IN-35
  • 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-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-152236

    Histone Methyltransferase Apoptosis Cancer
    PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor with an IC50 value of 192 nM. PRMT6-IN-3 can induce apoptosis in cancer cells and has anticancer activity .
    PRMT6-IN-3
  • 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-134883

    Histone Methyltransferase Cancer
    PRMT5-IN-4 is a PRMT5 inhibitor. PRMT5-IN-4 is applicable for cancer research .
    PRMT5-IN-4
  • HY-155050

    Apoptosis Histone Methyltransferase Cancer
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
    PRMT5-IN-31
  • 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-158143

    Histone Methyltransferase Cancer
    PRMT5-IN-34 (Compound C) is an inhibitor of MTA-cooperative Protein arginine methyltransferase 5 (PRMT5/MAT) .
    AZD3470
  • 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-174983

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-6 (Compound 31) is a selective MTA-cooperative PRMT5 inhibitor. PRMT5-MTA-IN-6 exhibits potent inhibitory activity against PRMT5・MTA (IC50: 6.6 nM). PRMT5-MTA-IN-6 selectively inhibits the growth of MTAP-deleted HCT-116 cells (IC50: 319 nM). PRMT5-MTA-IN-6 can be used in the research of MTAP-deleted tumors .
    PRMT5-MTA-IN-6
  • 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-176231

    Histone Methyltransferase Cancer
    PRMT5-IN-51 (compound 16–19F) is a potent PRMT5 inhibitor. PRMT5-IN-51 shows antiproliferative activity .
    PRMT5-IN-51
  • HY-178028

    Histone Methyltransferase Cancer
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
    PRMT5-IN-53
  • HY-176702

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-5 (Compound 7) is an orally active, irreversible PRMT5-MTA complex (PRMT5•MTA) inhibitor (IC50=1.15 nM). PRMT5-MTA-IN-5 blocks arginine methylation and inhibits ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-5 potently inhibits proliferation in MTAP-deficient tumor cells. PRMT5-MTA-IN-5 is promising for research of MTAP-deficient solid tumors, such as liver, breast, and pancreatic cancers .
    PRMT5-MTA-IN-5
  • HY-168263

    Histone Methyltransferase Apoptosis Cancer
    PRMT5-IN-45 (compound 36) is a potent and selective PRMT5 inhibitor with an IC50 of 3 nM. PRMT5-IN-45 potently reduces the level of symmetric dimethylarginines (sDMA) and inhibits the proliferation of MOLM-13 cell lines by inducing apoptosis and cell cycle arrest .
    PRMT5-IN-45
  • 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-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-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-162003A

    Histone Methyltransferase Cancer
    DCPT1061 hydrochloride has a strong inhibitory effect on PRMT1, PRMT6, and PRMT8 in vitro, The epigenetic enzymes such as PRMT3, PRMT4 and PRMT5 had little inhibitory effect. DCPT1061 hydrochloride has antitumor effects .
    DCPT1061 hydrochloride
  • 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-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-178274

    Histone Methyltransferase Apoptosis Cancer
    SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research .
    SKLB06329
  • 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-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-159732

    Histone Methyltransferase Cancer
    PRMT3-IN-4 (intermediate 15) is a protein arginine methyltransferase 3 (PRMT3) inhibitor. PRMT3-IN-4 is an active control for HY-19715. PRMT3-IN-4 can be used to synthesize PROTACs targeting PRMT3. PRMT3-IN-4 can be used in leukemia-related research .
    PRMT3-IN-4
  • HY-171132

    Histone Methyltransferase
    PRMT3-IN-5 (Compound 14) is an allosteric PRMT3 inhibitor (IC50: 291 nM). PRMT3-IN-5 can be used for investigating PRMT3's biological functions and disease associations .
    PRMT3-IN-5
  • HY-163592

    Histone Methyltransferase Cancer
    PRMT5-IN-43 (compound 4A) is a PRMT5 inhibitor. PRMT5-IN-43 can be used in cancer research .
    PRMT5-IN-43
  • HY-163593

    Histone Methyltransferase Cancer
    PRMT5-IN-44 (compound 12) is a PRMT5 inhibitor. PRMT5-IN-44 can be used in cancer research .
    PRMT5-IN-44

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