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Results for "

H3K4

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Apoptosis (9) Epigenetic Reader Domain (3) Fungal (1) Histone Demethylase (26) Histone Methyltransferase (12) Interleukin Related (1) NF-κB (1) Parasite (1) PD-1/PD-L1 (1) PROTACs (1) TNF Receptor (1) WDR5 (1)
By Research Areas:	Cancer (37) Infection (2) Inflammation/Immunology (3) Neurological Disease (2)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P2255

H3K4(Me) (1-20)	Histone Demethylase	Others
H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .

HY-122635A

T-448	Histone Demethylase	Neurological Disease
T-448 is a specific, orally active and irreversible inhibitor of *lysine-specific demethylase 1 (LSD1, an H3K4* demethylase), with an IC₅₀** of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .

HY-101938

Sinefungin 3 Publications Verification Adenosyl-Ornithine; A-9145; Antibiotic 32232RP	Histone Methyltransferase Fungal Antibiotic Parasite	Infection Inflammation/Immunology
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication . Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation .

HY-114209

MRK-740	Histone Methyltransferase	Cancer
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC₅₀ of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC₅₀ = 0.8 µM) .

HY-100869B

MM-589 (racemic mixture ) (TFA)	Histone Methyltransferase	Cancer
MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC₅₀ of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC₅₀ of 12.7 nM .

HY-19554A

MM-401 TFA 1 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
MM-401 (TFA) is a *MLL1 H3K4* methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis** and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-122635

T-448 free base	Histone Demethylase	Neurological Disease
T-448 free base is a specific, orally active and irreversible inhibitor of *lysine-specific demethylase 1 (LSD1, an H3K4* demethylase), with an IC₅₀** of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .

HY-19554

MM-401	Histone Methyltransferase Apoptosis	Cancer
MM-401 is a *MLL1 H3K4* methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis** and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-102047

KDOAM-25	Histone Demethylase	Cancer
KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .

HY-102047A

KDOAM-25 trihydrochloride	Histone Demethylase	Cancer
KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .

HY-102047B

KDOAM-25 citrate 5 Publications Verification	Histone Demethylase	Cancer
KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .

HY-16993

OICR-9429 Maximum Cited Publications 8 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .

HY-100869

MM-589	Histone Methyltransferase	Cancer
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC₅₀ of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC₅₀ of 12.7 nM .

HY-100869A

MM-589 TFA	Histone Methyltransferase	Cancer
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC₅₀ of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC₅₀ of 12.7 nM .

HY-109169

Bomedemstat IMG-7289	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-109169B

Bomedemstat hydrochloride IMG-7289 hydrochloride	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-109169C

Bomedemstat dihydrochloride IMG-7289 dihydrochloride	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-109169A

Bomedemstat ditosylate IMG-7289 ditosylate	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-151190

cis-4-Br-2,5-F2-PCPA S1024	Histone Demethylase	Cancer
cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a K_i value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells .

HY-141677B

INCB059872 tosylate	Histone Demethylase	Cancer
INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .

HY-122746

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 .

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-12220

MM-102 4 Publications Verification HMTase Inhibitor IX	Histone Methyltransferase Apoptosis NF-κB TNF Receptor Interleukin Related	Inflammation/Immunology Cancer
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC₅₀=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an *H3K4* histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .

HY-128912

Arborinine	Histone Demethylase	Cancer
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .

HY-138691

JQKD82 JADA82; PCK82	Histone Demethylase	Cancer
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma .

HY-138691A

JQKD82 trihydrochloride JADA82 trihydrochloride; PCK82 trihydrochloride	Histone Demethylase	Cancer
JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .

HY-138691B

JQKD82 dihydrochloride JADA82 dihydrochloride; PCK82 dihydrochloride	Histone Demethylase	Cancer
JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .

HY-168086

LSD1-IN-35	PD-1/PD-L1 Histone Demethylase	Infection Inflammation/Immunology
LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC₅₀: 108 nM). LSD1-IN-35 inhibits the demethylation on *H3K4me1/2*. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .

HY-149091

KDM5B-IN-4	Others	Cancer
KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC₅₀ of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .

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-P10819

S9-CMC1 TFA	Histone Demethylase Apoptosis	Cancer
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .

HY-100421

CPI-455 5+ Cited Publications	Histone Demethylase	Cancer
CPI-455 is a specific, pan-KDM5 inhibitor with an IC₅₀ of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .

HY-100421A

CPI-455 hydrochloride	Histone Demethylase	Cancer
CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC₅₀ of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .

HY-100764

YUKA1	Histone Demethylase	Cancer
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC₅₀ of 2.66 μM, less active on KDM5C (IC₅₀, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity .

HY-120400

KDM5-C70 3 Publications Verification	Histone Demethylase	Cancer
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .

HY-150619

KDM4-IN-4	Histone Demethylase	Cancer
KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC₅₀ value of 105 μM. KDM4-IN-4 can be used for researching anticancer .

HY-125837A

MS31 trihydrochloride	Epigenetic Reader Domain	Cancer
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC₅₀=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (K_d=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells .

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-125837

MS31	Epigenetic Reader Domain	Cancer
MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC₅₀=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (K_d=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells .

HY-100014

KDM5A-IN-1 2 Publications Verification	Histone Demethylase	Cancer
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC₅₀s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC₅₀ value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .

HY-158432

GT-653	Histone Demethylase PROTACs	Cancer
GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))

HY-151192

LSD1/2-IN-3	Histone Demethylase	Cancer
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a K_i value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation .

Cat. No.	Product Name	Target	Research Area

HY-P2257

H3K4(Me3) (1-20)	Peptides	Others
H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .

HY-P2255

H3K4(Me) (1-20)	Histone Demethylase	Others
H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .

HY-P2256

H3K4(Me2) (1-20) 1 Publications Verification	Peptides	Others
H3K4(Me2) (1-20) is a histone peptide. H3K4me2 regulates the recovery of protein biosynthesis and homeostasis following DNA damage .

HY-19554

MM-401	Histone Methyltransferase Apoptosis	Cancer
MM-401 is a *MLL1 H3K4* methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC₅₀ = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis** and differentiation. MM-401 can be used for the research of MLL leukemia .

HY-P10819

S9-CMC1 TFA	Histone Demethylase Apoptosis	Cancer
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-128912

Arborinine	Structural Classification Alkaloids Animals Source classification	Histone Demethylase
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .

Cat. No.	Compare	Product Name	Species	Source

HY-P76062

	SETD7 Protein, Human (His) Histone-lysine N-methyltransferase SETD7; H3-K4-HMTase SETD7; SET7/9; KIAA1717; KMT7; SET7; SET9	Human	E. coli
	The SETD7 protein is a histone methyltransferase that specifically monomethylates H3K4, a mark associated with transcriptional activation. Its role in gene activation extends to the collagenase and insulin genes, specifically at the insulin promoter when IPF1/PDX-1 is recruited. SETD7 Protein, Human (His) is the recombinant human-derived SETD7 protein, expressed by E. coli , with N-His labeled tag. The total length of SETD7 Protein, Human (His) is 365 a.a., with molecular weight of 47-50 kDa.

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HY-P80531

	Acetyl-Histone H3 (Lys4) Antibody H3K4ac; H3/j; H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3FJ; H3C10; H3C11; HIST1H3J	WB, ICC/IF	Human, Mouse
	Acetyl-Histone H3 (Lys4) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 15 kDa, targeting to Acetyl-Histone H3 (Lys4). It can be used for WB,ICC/IF assays with tag free, in the background of Human, Mouse.

HY-P83151

	SETD7 Antibody (YA2896) Histone H3-K4 methyltransferase SETD7; Lysine N-methyltransferase 7; SET domain-containing protein 7; SET7; SET9	WB, IP	Human, Mouse, Rat
	SETD7 Antibody (YA2896) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2896), targeting SETD7, with a predicted molecular weight of 41 kDa (observed band size: 41 kDa). SETD7 Antibody (YA2896) can be used for WB, IP experiment in human, mouse, rat background.

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H3K4

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