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Results for "

histone lysine methyltransferases

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DNA Methyltransferase (1) Histone Demethylase (2) Histone Methyltransferase (19) Aldehyde Dehydrogenase (ALDH) (1) Apoptosis (5) Autophagy (3) Chemerin Receptor (1) Cholinesterase (ChE) (1) SARS-CoV (1)
By Research Areas:	Cancer (21) Infection (1) Inflammation/Immunology (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Histone Methyltransferase Histone Demethylase Histone Acetyltransferase HDAC DNA Methyltransferase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-44062

G9a-IN-1	Histone Methyltransferase	Inflammation/Immunology Cancer
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .

HY-12991A

BIX-01338 hydrate	Histone Methyltransferase	Cancer
BIX-01338 hydrate is a **histone lysine methyltransferase** inhibitor.

HY-122182

OTS193320	Histone Methyltransferase Apoptosis	Cancer
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .

HY-135128

Dot1L-IN-5 1 Publications Verification	Histone Methyltransferase	Cancer
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC₅₀ of 0.17 nM .

HY-135127

Dot1L-IN-4	Histone Methyltransferase	Cancer
Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.11 nM .

HY-10587A

BIX-01294 hydrochloride hydrate	Histone Methyltransferase Apoptosis Autophagy	Cancer
BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC₅₀ of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells .

HY-135129

Dot1L-IN-6	Histone Methyltransferase	Cancer
Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.19 nM .

HY-116971

DCG066	Histone Methyltransferase Apoptosis	Cancer
DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .

HY-113786

EZH2-IN-21	Histone Methyltransferase	Cancer
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .

HY-156455

SETD7-IN-1	Histone Methyltransferase	Cancer
SETD7-IN-1 (compound 7) is a PFI-2 (HY-18627) analogue. SETD7-IN-1 is a substrate and inhibitor of histone lysine methyltransferase SETD7, with an IC₅₀ of 0.96 ± 0.10 µM .

HY-116605

GSK926	Histone Methyltransferase	Cancer
GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC₅₀=0.02 μM; K_i=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research .

HY-111544

EML741	Histone Methyltransferase	Cancer
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC₅₀ of 23 nM, K_d of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC₅₀, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .

HY-16705

BRD4770 3 Publications Verification	Histone Methyltransferase	Cancer
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC₅₀ of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .

HY-125244

LEM-14-1189	Histone Methyltransferase	Cancer
LEM-14-1189, a LEM-14 (HY-114340) derivative, is a NSDs inhibitor with IC₅₀s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research .

HY-156285

ZZM-1220	Histone Methyltransferase Apoptosis	Cancer
ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC₅₀s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .

HY-150680

SARS-CoV-2 nsp14-IN-1	SARS-CoV Histone Methyltransferase DNA Methyltransferase	Infection
SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC₅₀ value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases .

HY-P10463

ssK36	Histone Methyltransferase	Cancer
ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. It is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .

HY-10587

BIX-01294 Maximum Cited Publications 23 Publications Verification	Histone Methyltransferase Autophagy	Cancer
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells .

HY-108239

BIX-01294 trihydrochloride	Histone Methyltransferase Autophagy	Cancer
BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells .

HY-138097

α-NETA 5+ Cited Publications	Chemerin Receptor Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis	Cancer
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity .

HY-146283

LSD1-IN-18	Histone Demethylase	Cancer
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.156 μM and K_D of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC₅₀ (72 h) of 0.16 and 0.21 μM, respectively .

HY-146284

LSD1-IN-19	Histone Demethylase	Cancer
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.108 μM and K_D of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC₅₀ (72 h) of 0.17 and 0.40 μM, respectively .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library	621 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 621 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

621 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 621 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-P10463

ssK36	Histone Methyltransferase	Cancer
ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. It is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .

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