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histone H3K9

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By Targets:	HDAC (4) Histone Demethylase (1) Histone Methyltransferase (10) Apoptosis (4) Autophagy (1) Sirtuin (1)
By Research Areas:	Cancer (12) Inflammation/Immunology (2) Neurological Disease (3)

14

Inhibitors & Agonists

2

Peptides

1

Antibodies

Targets Recommended: Histone Methyltransferase Histone Demethylase Histone Acetyltransferase HDAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

BRD6688	HDAC	Neurological Disease
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .

cis-BG47	HDAC Histone Methyltransferase	Neurological Disease
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases **Histone Methyltransferase H3K9** acetylation. cis-BG47 can be used for neurological disease research .

BRD4770 2 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 .

E67-2	Histone Methyltransferase	Cancer
E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC₅₀ value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .

JMJD3/HDAC-IN-1	HDAC Histone Demethylase Apoptosis	Cancer
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC₅₀=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .

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 .

UNC 0631 2 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 .

MDL-811	Sirtuin	Cancer
MDL-811, an allosteric SIRT6 activator, significantly activates SIRT6 histone H3 deacetylation (H3K9Ac, H3K18Ac, and H3K56Ac). MDL-811 could be used in the study of colorectal cancer .

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 .

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 .

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 .

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 .

HDAC2-IN-1	HDAC	Neurological Disease
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC₅₀ of 0.5 μM . HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC₅₀s of 1.61 μM and 0.98 μM, respectively .

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 .

Cat. No.	Product Name	Target	Research Area

Histone H3K9me3 (1-15) (TFA) H3(1-15)K9me3 TFA	Peptides	Others
Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as substrate. Histone H3K9me3 is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin .

Histone H3K9me3 (1-15) H3(1-15)K9me3	Peptides	Inflammation/Immunology Cancer
Histone H3K9me3 (1-15) (H3(1-15)K9me3) is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin. Trimethylation of histone H3 at lysine 9 is associated with gene repression, prevents transcription factor binding .

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