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Isoforms Recommended:	EHMT2/G9a/KMT1C

Results for "

G9A

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aldehyde Dehydrogenase (ALDH) (1) Apoptosis (6) Autophagy (5) Chemerin Receptor (1) Cholinesterase (ChE) (1) DNA Methyltransferase (3) Epigenetic Reader Domain (1) GCGR (1) GLP Receptor (2) Histone Demethylase (1) Histone Methyltransferase (34) Influenza Virus (2) PROTACs (2) VSV (2) WDR5 (1)
By Research Areas:	Cancer (33) Infection (2) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (1)

Inhibitors & Agonists

Peptides

Antibodies

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-120444

MS0124	Histone Methyltransferase	Cancer
MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC₅₀ values of 13±4 nM and 440±63 nM for GLP and G9a,respectively .

HY-162362

MS8709	PROTACs GLP Receptor	Cancer
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class *G9a/GLP* PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .

HY-100757

CPUY074020	Histone Methyltransferase	Cancer
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase *G9a, with an IC₅₀* of 2.18 μM. CPUY074020 possesses anti-proliferative activity .

HY-13807

UNC0646 1 Publications Verification	Histone Methyltransferase	Cancer
UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC₅₀ of 6 nM. UNC0646 is also a potent GLP inhibitor (IC₅₀ <15 nM) and highly selective for *G9a/GLP* over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces *H3K9me2* levels in MDA-MB-231 cells with an IC₅₀ of 26 nM .

HY-15647

BRD9539 1 Publications Verification	Histone Methyltransferase	Cancer
BRD9539 is a histone methyltransferase G9a inhibitor with an IC₅₀ of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .

HY-161787

G9a-IN-2	Histone Methyltransferase	Others
G9a-IN-2 (Compound 7i) is an inhibitor for histone methyltransferases *G9a* with IC₅₀ of 0.024 μM. G9a-IN-2 reduces H3K9me2 levels and induces the mRNA expression of γ-globin mRNA. G9a-IN-2 shows the potential in ameliorating sickle cell disease (SCD) .

HY-133031A

CSV0C018875 hydrochloride	Histone Methyltransferase	Others
CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .

HY-155020

Antitumor agent-101	Histone Methyltransferase GLP Receptor	Cancer
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC₅₀s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .

HY-133031

CSV0C018875	Histone Methyltransferase	Cancer
CSV0C018875 is a quinoline-based *EHMT2/G9a* inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294 .

HY-101925

CM-272 3 Publications Verification	Histone Methyltransferase DNA Methyltransferase Apoptosis	Cancer
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits *G9a, DNMT1, DNMT3A, DNMT3B* and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .

HY-13808

UNC 0631 3 Publications Verification	Histone Methyltransferase	Cancer
UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC₅₀ of 4 nM. UNC 0631 potently reduces *H3K9me2* levels in MDA-MB-231 cells with an IC₅₀ of 25 nM .

HY-13980

UNC0642 15+ Cited Publications	Histone Methyltransferase	Cancer
UNC0642 is a potent and selective lysine methyltransferases *G9a* and GLP inhibitor, with an IC₅₀ of <2.5 nM for *G9a*.

HY-117421A

CM-579 trihydrochloride	Histone Methyltransferase DNA Methyltransferase	Cancer
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of *G9a* and DNMT, with IC₅₀ values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .

HY-117421

CM-579	Histone Methyltransferase DNA Methyltransferase	Cancer
CM-579 is a first-in-class reversible, dual inhibitor of *G9a* and DNMT, with IC₅₀ values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .

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-10930

UNC0321 2 Publications Verification	Histone Methyltransferase GCGR Apoptosis	Cancer
UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a K_i of 63 pM and with assay-dependent IC₅₀ values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC₅₀ values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .

HY-152775A

RK-0133114	Histone Methyltransferase	Metabolic Disease
RK-0133114 is a *G9a* inhibitor and a R-enantiomer of RK-701 (HY-152775). RK-0133114 inhibits G9a with an IC₅₀ value of 3.7 μM. RK-0133114 can be used for the research of sickle cell disease (SCD) .

HY-10929

UNC0224 2 Publications Verification	Histone Methyltransferase	Cancer
UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a K_i of 2.6 nM, an IC₅₀ of 15 nM and a K_d of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC₅₀ values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .

HY-118715

Setin-1	Histone Methyltransferase	Cancer
Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a .

HY-150510

MS8511	Histone Methyltransferase	Neurological Disease Cancer
MS8511 is a selective *G9a/GLP* covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC₅₀ values of 100 nM (G9a) and 140 nM (GLP), and K_d values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .

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-110093

UNC0638 hydrate	VSV Histone Methyltransferase Autophagy Influenza Virus	Infection Cancer
UNC0638 hydrate selectively inhibits *G9a* and GLP histone methyltransferases with IC₅₀ of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .

HY-164479

GA001	Histone Methyltransferase Autophagy Apoptosis	Cancer
GA001 is a potent *G9a* antagonist, with an IC₅₀ of 1.32 μM. GA001 induces autophagy and apoptosis that can be used for the breast cancer .

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-162749

G9D-4	PROTACs Histone Methyltransferase	Cancer
G9D-4 is a potent PROTAC degrader of *G9a, with the DC₅₀* value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC₅₀ of ＞10 μM. G9D-4 plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)) .

HY-161759

MS152	Histone Methyltransferase	Metabolic Disease
MS152 is an oral bioactive inhibitor of *EHMT2/G9a*. MS152 reactivats maternally silenced Prader-Willi syndrome (PWS) genes in brain and liver tissues of PWS mouse models .

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-12583

A-366 3 Publications Verification	Histone Methyltransferase Epigenetic Reader Domain	Cancer
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase *G9a* inhibitor with IC₅₀s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC₅₀=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (K_i=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .

HY-121093

DC-S239	Histone Methyltransferase	Cancer
DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC₅₀ value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .

HY-152775

RK-701	Histone Methyltransferase	Cancer
RK-701 is an highly selective and non-genotoxic inhibitor of *G9a* with IC₅₀ value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A .

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-146285

LSD1-IN-20	Histone Demethylase Histone Methyltransferase	Cancer
LSD1-IN-20 (compound 1) is a potent dual non-covalent *LSD1/G9a* inhibitor, with K_i values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC₅₀ (72 h) of 0.51 and 1.60 μM, respectively .

HY-148817

WDR5-0102	WDR5	Cancer
WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (K_dis=7 μM, K_d=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5 .

HY-15273

UNC0638 5+ Cited Publications	VSV Histone Methyltransferase Autophagy Influenza Virus	Infection Cancer
UNC0638 selectively inhibits *G9a* and GLP histone methyltransferases with IC₅₀ of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .

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 .

Cat. No.	Product Name	Target	Research Area

HY-P2554

Histone H3 (1-25), amide	Peptides	Others
Histone H3 (1-25), amide is an N-terminal peptide fragment of histone H3. Histone H3 (1-25), amide can be used to identify the substrate for histone methyltransferases (HMTs). Histone H3 (1-25), amide, as a substrate for HMT G9a, shows more efficient than histone H3 (15-39) and full-length histone H3 .

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P82628

	EHMT2 Antibody (YA2373) Bat8; Ehmt2; G9A; GAT8; NG36	WB, IHC-P	Human
	EHMT2 Antibody (YA2373) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2373), targeting EHMT2, with a predicted molecular weight of 132 kDa (observed band size: 170 kDa). EHMT2 Antibody (YA2373) can be used for WB, IHC-P experiment in human background.

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