2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. PRMT5 Isoform
  6. PRMT5 Inhibitor

PRMT5 Inhibitor

PRMT5 Inhibitors (44):

Cat. No. Product Name Effect Purity
  • HY-101563
    GSK3326595
    		Inhibitor 99.83%
    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.
  • HY-139611
    Navlimetostat
    		Inhibitor 99.40%
    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.
  • HY-12727
    EPZ015666
    		Inhibitor 99.83%
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
  • HY-101564
    Onametostat
    		Inhibitor 99.79%
    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.
  • HY-100235
    GSK591
    		Inhibitor 99.91%
    GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
  • HY-176534
    PRMT5-IN-52
    		Inhibitor
    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.
  • HY-176701
    PRMT5-MTA-IN-4
    		Inhibitor
    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.
  • HY-176702
    PRMT5-MTA-IN-5
    		Inhibitor
    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.
  • HY-107777
    LLY-283
    		Inhibitor 99.22%
    LLY-283 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.
  • HY-148419
    Ralometostat
    		Inhibitor 99.90%
    TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research.
  • HY-131493
    PF-06939999
    		Inhibitor 99.84%
    PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect.
  • HY-124131
    DS-437
    		Inhibitor 99.22%
    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.
  • HY-138684
    MRTX9768
    		Inhibitor 99.60%
    MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.
  • HY-148674
    PRMT5-IN-25
    		Inhibitor 99.94%
    PRMT5-IN-25 (compound 503) is a potent PRMT5 inhibitor with an Ki value of 0.06 nM. PRMT5-IN-25 shows antiproliferative.
  • HY-100025A
    HLCL-61 hydrochloride
    		Inhibitor 99.87%
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
  • HY-139611C
    Navlimetostat hydrochloride
    		Inhibitor 99.22%
    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.
  • HY-132309
    BRD0639
    		Inhibitor 98.04%
    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.
  • HY-Q36691
    PRMT5-IN-30
    		Inhibitor 99.17%
    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.
  • HY-120137
    CMP-5
    		Inhibitor 99.61%
    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.
  • HY-109963
    PR5-LL-CM01
    		Inhibitor 98.37%
    PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.