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arginine methylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Biochemical Assay Reagents (1) Discoidin Domain Receptor (1) Epigenetic Reader Domain (1) Fungal (1) Histone Acetyltransferase (1) Histone Methyltransferase (12) LYTACs (1) PROTACs (2) Sirtuin (1)
By Research Areas:	Cancer (13) Infection (1) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: SRPK Protein Arginine Deiminase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128717A

GSK3368715 dihydrochloride Maximum Cited Publications 18 Publications Verification 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 .

HY-128717

GSK3368715 Maximum Cited Publications 18 Publications Verification 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 .

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-156152A

CARM1 degrader-1 hydrochloride	PROTACs Histone Methyltransferase	Cancer
CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC₅₀ = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research .

HY-156152

CARM1 degrader-1	PROTACs Histone Methyltransferase	Cancer
CARM1 degrader-1 is a CARM1 PROTAC degrader (DC₅₀ = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer .

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-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-P2556

Histone H3 (21-44)	Biochemical Assay Reagents	Others
Histone H3 (21-44), derived from histone H3 21-44 amino acids, is usually used as a substrate (such as protein arginine methyltransferases) for methylation assays .

HY-153421

PRMT5-IN-28	Histone Methyltransferase	Cancer
PRMT5-IN-28 (compound 36) is an inhibitor of *protein arginine* methyltransferase 5 (PRMT5*) enzyme. Protein arginine* methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape .

HY-W013500

(1-Nitroethene-1,2-diyl)dibenzene alpha-Nitrostilbene; α-Nitrostilbene; NSC 385	Histone Methyltransferase	Others
(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC₅₀=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.

HY-128717C

GSK3368715 hydrochloride EPZ019997 hydrochloride	Histone Methyltransferase	Cancer
GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC₅₀ values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity .

HY-128717B

GSK3368715 trihydrochloride EPZ019997 trihydrochloride	Histone Methyltransferase	Cancer
GSK3368715 trihydrochloride (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 trihydrochloride (EPZ019997) produces a shift in arginine* methylation states, alters exon usage, and has strong anti-cancer activity .

HY-172732

PRMT5-IN-50	Histone Methyltransferase	Cancer
PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC₅₀s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice .

HY-183061

MrTAC-8	LYTACs Epigenetic Reader Domain	Neurological Disease Cancer
MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC₅₀ values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma .

HY-114510

PRMT/HKMT-IN-1	Discoidin Domain Receptor Histone Acetyltransferase Sirtuin Fungal Apoptosis	Infection Cancer
PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC₅₀ of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library	904 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 904 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Histone Modification Research Compound Library

904 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 904 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Cat. No.	Product Name	Target	Research Area

HY-P2556

Histone H3 (21-44)	Biochemical Assay Reagents	Others
Histone H3 (21-44), derived from histone H3 21-44 amino acids, is usually used as a substrate (such as protein arginine methyltransferases) for methylation assays .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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