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PRMTs

" in MedChemExpress (MCE) Product Catalog:

191

Inhibitors & Agonists

1

Peptides

2

Natural
Products

3

Isotope-Labeled Compounds

25

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-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-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-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-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-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-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
  • HY-163587

    Histone Methyltransferase Cancer
    PRMT5-IN-39-d3 is the deuterated form of PRMT5-IN-39. PRMT5-IN-39-d3 is an orally active PRMT5 inhibitor and can be used for study of cancer .
    PRMT5-IN-39-d3
  • HY-163591

    Histone Methyltransferase Cancer
    PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research .
    PRMT5-IN-36-d3
  • 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-168842

    Histone Methyltransferase Cancer
    PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity .
    PRMT5-IN-47
  • HY-115758

    Histone Methyltransferase Cancer
    PRMT1-IN-1 is a PRMT1 inhibitor.
    PRMT1-IN-1
  • 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-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-160029

    Histone Methyltransferase Cancer
    PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM .
    PRMT5-IN-32
  • 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-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-146810

    Histone Methyltransferase Cancer
    PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC50=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability .
    PRMT4-IN-1
  • 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-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-153422

    Histone Methyltransferase Cancer
    PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research .
    PRMT5-IN-29
  • HY-162230

    Apoptosis Histone Methyltransferase Cancer
    PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity .
    PRMT5-IN-33
  • 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-19615B
    MS023 dihydrochloride
    15+ 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-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-170603

    Fluorescent Dye Histone Methyltransferase Apoptosis Cancer
    PRMT5-targeted fluorescent ligand-1 (Compound 7) is a PRMT5-targeted fluorescent ligand, that inhibits PRMT5 with an IC50 of 29.39 nM. PRMT5-targeted fluorescent ligand-1 exhibits cell imaging activity, that exhibits good fluorescence signal in MCF-7 with an IC50 of 29 nM. PRMT5-targeted fluorescent ligand-1 induces apoptosis. PRMT5-targeted fluorescent ligand-1 exhibits a maximal excitation wavelength of 438 nm and a maximal emission wavelength of 550 nm .
    PRMT5-targeted fluorescent ligand-1
  • HY-141874

    Histone Methyltransferase Cancer
    PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5.
    PRMT5-IN-12
  • HY-163590

    Histone Methyltransferase Potassium Channel Cancer
    PRMT5-IN-41 (compound 130) is a potent and orally active PRMT5 inhibitor. PRMT5-IN-41 inhibits hERG ion channel with IC50 value of 1.36 µM .
    PRMT5-IN-41
  • 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-144189

    Histone Methyltransferase Cancer
    PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5, such as cancer .
    PRMT5-IN-18
  • HY-158143

    Histone Methyltransferase Cancer
    PRMT5-IN-34 (Compound C) is an inhibitor of MTA-cooperative Protein arginine methyltransferase 5 (PRMT5/MAT) .
    PRMT5-IN-34
  • HY-139823

    Histone Methyltransferase Others
    PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
    PRMT5-IN-10
  • 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-19615
    MS023
    15+ 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-163799

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
    PRMT5-MTA-IN-1
  • HY-142211

    Histone Methyltransferase Cancer
    PRMT5-IN-15 is a PRMT5 inhibitor with an IC50 value of 0.84 nM.
    PRMT5-IN-15
  • HY-163589

    Histone Methyltransferase Others
    PRMT5-IN-40 (compound 104) is a potent inhibitor of PRMT5 .
    PRMT5-IN-40
  • HY-149005

    Histone Methyltransferase Cancer
    PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
    PRMT5-IN-19
  • HY-153057

    Histone Methyltransferase Metabolic Disease Cancer
    PRMT5-IN-46 (compound 278) inhibits PRMT5 with IC50s of 1-10 μM. PRMT5 is a methyltransferase which is associated with specific genetic alterations. PRMT5-IN-46 can be used for research of proliferative diseases, metabolic disorders, and blood diseases .
    PRMT5-IN-46
  • 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

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