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PRMT5 Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) Akt (2) Androgen Receptor (1) Apoptosis (16) Bcl-2 Family (3) BCL6 (1) Caspase (2) CDK (2) COX (2) Cytochrome P450 (2) Drug Metabolite (1) EGFR (1) ERK (2) Fluorescent Dye (1) HDAC (1) Histone Demethylase (2) Histone Methyltransferase (108) IAP (2) Isotope-Labeled Compounds (1) JNK (2) KLF (2) MDM-2/p53 (2) NO Synthase (2) p38 MAPK (2) PAK (1) Parasite (3) Phosphodiesterase (PDE) (3) PI3K (2) Potassium Channel (2) PROTACs (3) Reference Standards (8) SARS-CoV (2) Survivin (2)
By Research Areas:	Cancer (109) Infection (5) Inflammation/Immunology (7) Metabolic Disease (1)
Oligonucleotides:	Aptamers (2)

112

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

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 .

HY-101564

Onametostat 5+ Cited Publications JNJ-64619178	Histone Methyltransferase	Cancer
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-153390

AMG-193	Histone Methyltransferase	Cancer
AMG 193 is an orally active MTA-cooperative *PRMT5* inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting *PRMT5* (IC₅₀=0.107 μM), thereby protecting normal cells with wild-type MTAP .

HY-156680

Vopimetostat TNG-462	Histone Methyltransferase	Cancer
TNG-462 is an orally active and selective *PRMT5* inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers .

HY-12727

EPZ015666 20+ Cited Publications GSK3235025	Histone Methyltransferase	Cancer
EPZ015666 (GSK3235025) is an orally available inhibitor of *PRMT5* with an IC₅₀ of 22 nM.

HY-100235

GSK591 10+ Cited Publications EPZ015866; GSK3203591	Histone Methyltransferase	Cancer
GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC₅₀ of 4 nM .

HY-148419

Ralometostat 2 Publications Verification TNG908	Histone Methyltransferase	Cancer
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 PRMT5-IN-3	Histone Methyltransferase Apoptosis	Cancer
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-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 K_d of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity .

HY-N2420

Flavokawain A 2 Publications Verification	Apoptosis Histone Methyltransferase Cytochrome P450 Caspase Survivin IAP p38 MAPK PI3K NO Synthase COX JNK ERK Akt	Inflammation/Immunology Cancer
Flavokawain A is a chalcone compound and an orally active inhibitor of *PRMT5* and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer .

HY-138684

MRTX9768	Histone Methyltransferase	Cancer
MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .

HY-100025A

HLCL-61 hydrochloride 2 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).

HY-141877

MS4322 1 Publications Verification YS43-22	PROTACs Histone Methyltransferase	Cancer
MS4322 (YS43-22) is a specific *PRMT5* PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC₅₀ of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC₅₀ of 18 nM. MS4322 promotes ubiquitination and degradation of *PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5* ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .

HY-111213

PRMT5-IN-20	Histone Methyltransferase	Cancer
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity .

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 .

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 .

HY-151576

PRMT5:MEP50 PPI	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 .

HY-112165

PRMT5-IN-2	Histone Methyltransferase	Cancer
PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3 .

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 .

HY-163588

GTA182 PRMT5-IN-39	Histone Methyltransferase	Cancer
GTA182 (compound 107) is an orally active *PRMT5* inhibitor and can be used for study of cancer .

HY-148674

AM-9747	Histone Methyltransferase	Cancer
AM-9747 (compound 503) is a potent *PRMT5* inhibitor with an K_i value of 0.06 nM. AM-9747 shows antiproliferative .

HY-Q36691

PRMT5-IN-30	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 K_d 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-109963

PR5-LL-CM01	Histone Methyltransferase	Cancer
PR5-LL-CM01 is a potent protein arginine methyltransferase 5 *(PRMT5)* inhibitor (IC₅₀= 7.5 μM). Anti-tumor activies .

HY-160865

PRMT5-IN-35	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 .

HY-126256A

PRMT5-IN-1 hydrochloride	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 .

HY-128579

DW14800	Histone Methyltransferase	Cancer
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC₅₀ of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity .

HY-141877B

MS4322 (isomer) YS43-22 (isomer)	PROTACs Histone Methyltransferase	Cancer
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific *PRMT5* PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC₅₀ of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC₅₀ of 18 nM. MS4322 promotes ubiquitination and degradation of *PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5* ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .

HY-139611B

(S)-Navlimetostat (S)-MRTX-1719; (S)-BMS-986504	Histone Methyltransferase	Cancer
(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a *PRMT5/MTA* complex inhibitor, with an IC₅₀ of 7070 nM .

HY-107777A

LLY-284	Histone Methyltransferase	Cancer
LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .

HY-134883

PRMT5-IN-4	Histone Methyltransferase	Cancer
PRMT5-IN-4 is a *PRMT5* inhibitor. PRMT5-IN-4 is applicable for cancer research .

HY-155050

PRMT5-IN-31	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 (T_1/2: 132.4 min) .

HY-126256

PRMT5-IN-1	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 .

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 .

HY-162783

AZ-PRMT5i-1	Histone Methyltransferase	Cancer
AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective *PRMT5* inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers .

HY-168263

PRMT5-IN-45	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 .

HY-176534

PRMT5-IN-52	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 .

HY-176231

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

HY-174983

PRMT5-MTA-IN-6	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 .

HY-178028

PRMT5-IN-53	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 K_D 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) .

HY-176702

PRMT5-MTA-IN-5	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 .

HY-176701

PRMT5-MTA-IN-4	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 .

HY-144189

PRMT5-IN-18	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 .

HY-141876

PRT543	Histone Methyltransferase	Cancer
PRT543 is a *PRMT5* inhibitor to research cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

HY-160029

PRMT5-IN-32	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 .

HY-169218

WK692	BCL6	Cancer
WK692 is a BCL6 inhibitor that inhibits the BCL6 ^BTB/SMRT interaction. WK692 can effectively inhibit the growth of diffuse large B-cell lymphoma cells and synergize with EZH2 and PRMT5 inhibitors. .

HY-174908

SJL2-1	Histone Methyltransferase 11β-HSD Androgen Receptor	Cancer
SJL2-1 is a *PRMT5* inhibitor, with an IC₅₀ of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC) .

HY-144188

PRMT5-IN-17	Histone Methyltransferase	Cancer
PRMT5-IN-17 (Compound 6) is a *PRMT5* inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .

HY-144187

PRMT5-IN-16	Histone Methyltransferase	Cancer
PRMT5-IN-16 (Compound 20) is a *PRMT5* inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .

HY-N2420R

Flavokawain A (Standard)	Reference Standards Apoptosis Histone Methyltransferase Cytochrome P450 Caspase Survivin IAP p38 MAPK PI3K NO Synthase COX JNK ERK Akt	Inflammation/Immunology Cancer
Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer .

HY-163592

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

Cat. No.	Product Name	Target	Research Area

HY-P3822

PRMT5-IN-23	Histone Methyltransferase	Cancer
PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. *PRMT5* is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2420

Flavokawain A 2 Publications Verification	Chalcones Monophenols Flavonoids other families Classification of Application Fields Phenols Plants Disease Research Fields Source Classification Cancer	Apoptosis Histone Methyltransferase Cytochrome P450 Caspase Survivin IAP p38 MAPK PI3K NO Synthase COX JNK ERK Akt
Flavokawain A is a chalcone compound and an orally active inhibitor of *PRMT5* and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer .

HY-N2420R

Flavokawain A (Standard)	Structural Classification Chalcones Monophenols Flavonoids other families Phenols Plants Source Classification	Reference Standards Apoptosis Histone Methyltransferase Cytochrome P450 Caspase Survivin IAP p38 MAPK PI3K NO Synthase COX JNK ERK Akt
Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer .

Cat. No.	Product Name	Chemical Structure

HY-163587

PRMT5-IN-39-d3
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 .

HY-163591

PRMT5-IN-36-d3
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 .

HY-172733S

PRMT5-MTA-IN-3-d3

PRMT5-MTA-IN-3-d₃ (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d₃ is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d₃ has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC₅₀ values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d₃ has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .

Cat. No.	Product Name		Classification

HY-147081

AS 1411 2 Publications Verification AGRO-100		Aptamers
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .

HY-147081A

AS 1411 sodium 2 Publications Verification AGRO-100 sodium		Aptamers
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity

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