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Results for "

PRMT5+inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) Akt (1) Androgen Receptor (1) Apoptosis (8) Bcl-2 Family (1) BCL6 (1) CDK (2) DNA/RNA Synthesis (1) Histone Demethylase (1) Histone Methyltransferase (59) MDM-2/p53 (2) Notch (1) PI3K (1) Potassium Channel (1) Reference Standards (3) SARS-CoV (2)
By Research Areas:	Cancer (59) Infection (2) Inflammation/Immunology (1) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101563

GSK3326595 Maximum Cited Publications 31 Publications Verification EPZ015938	Histone Methyltransferase SARS-CoV MDM-2/p53 CDK Apoptosis	Infection Cancer
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 ^[5].

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-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-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-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-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-111213

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

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-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-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-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-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-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-134883

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

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-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-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-158143

AZD3470	Histone Methyltransferase Apoptosis	Cancer
AZD3470 is an orally active MTA-cooperative *PRMT5* inhibitor, selective for MTAP-deficient tumors. AZD3470 induces cell cycle G₂/M phase alterations, DNA damage, apoptosis, and symmetric dimethylarginine reduction. AZD3470 alters alternative splicing, increases skipped exon events in DNA repair and cell cycle pathways, and inhibits cancer cell proliferation and tumor growth. AZD3470 can be used for the research of non-small cell lung cancer and MTAP-deleted solid tumors .

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-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-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-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-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-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-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-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-141876

PRT543	Histone Methyltransferase Notch PI3K Akt Bcl-2 Family DNA/RNA Synthesis	Cancer
PRT543 is an orally active selective *PRMT5* inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia ^[5].

HY-142211

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

HY-150081

PRMT5-IN-21	Histone Methyltransferase	Cancer
PRMT5-IN-21 (compound 1) is a potent cyclonucleoside *PRMT5* inhibitor .

HY-132937

PRMT5-IN-9	Histone Methyltransferase	Cancer
PRMT5-IN-9 is a novel PRMT5 inhibitor for researching cancer, with an IC₅₀ of 0.01 μM.

HY-163585

PRMT5-IN-36	Histone Methyltransferase	Cancer
PRMT5-IN-36 (compound 4) is an orally active *PRMT5* inhibitor and can be used for study of cancer .

HY-163586

PRMT5-IN-37	Histone Methyltransferase	Cancer
PRMT5-IN-37 (compound 29) is an orally active *PRMT5* inhibitor and can be used for study of cancer .

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-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 .

HY-163593

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

HY-153422

PRMT5-IN-29	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 .

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-163590

PRMT5-IN-41	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 .

HY-163587

PRMT5-IN-39-d3	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 .

HY-163591

PRMT5-IN-36-d3	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 .

HY-168842

PRMT5-IN-47	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 .

HY-162230

PRMT5-IN-33	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 .

HY-153390A

(R)-AMG-193	Histone Methyltransferase	Cancer
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). 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-170792

PRMT5-IN-48	Histone Methyltransferase	Cancer
PRMT5-IN-48 (compound D3) is an orally effective *PRMT5* inhibitor (IC₅₀=20.7 nM) with anticancer activity. PRMT5-IN-48 can inhibit the growth of various cancer cells, induce apoptosis (apoptosis), and arrest the cell cycle at the G0/G1 phase. PRMT5-IN-48 can be used for non-Hodgkin lymphoma (NHL) research .

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 .

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 .

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