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Results for "

Histone+Methyltransferase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Methyltransferase (60) Antibiotic (1) Apoptosis (10) Autophagy (6) Bacterial (4) c-Myc (1) Caspase (1) CD38 (1) CD44 (1) Cholecystokinin Receptor (1) CRFR (2) Endogenous Metabolite (1) Epigenetic Reader Domain (2) Ferroportin (1) GCGR (1) HDAC (2) HOXA (1) Influenza Virus (2) Interleukin Related (1) Isotope-Labeled Compounds (2) Keap1-Nrf2 (1) MMP (1) NF-κB (1) Orthopoxvirus (4) Parasite (1) Reactive Oxygen Species (ROS) (1) Reference Standards (6) S-adenosylhomocysteine hydrolase (SAHH) (3) Sirtuin (1) TNF Receptor (1) Vasopressin Receptor (1) Virus Protease (1) VSV (2) WDR5 (7)
By Research Areas:	Cancer (59) Cardiovascular Disease (3) Infection (13) Inflammation/Immunology (8) Metabolic Disease (5) Neurological Disease (4)

By Targets:

Histone Methyltransferase (60)

Antibiotic (1)

Apoptosis (10)

Autophagy (6)

Bacterial (4)

c-Myc (1)

Caspase (1)

CD38 (1)

CD44 (1)

Cholecystokinin Receptor (1)

CRFR (2)

Endogenous Metabolite (1)

Epigenetic Reader Domain (2)

Ferroportin (1)

GCGR (1)

HDAC (2)

HOXA (1)

Influenza Virus (2)

Interleukin Related (1)

Isotope-Labeled Compounds (2)

Keap1-Nrf2 (1)

MMP (1)

NF-κB (1)

Orthopoxvirus (4)

Parasite (1)

Reactive Oxygen Species (ROS) (1)

Reference Standards (6)

S-adenosylhomocysteine hydrolase (SAHH) (3)

Sirtuin (1)

TNF Receptor (1)

Vasopressin Receptor (1)

Virus Protease (1)

VSV (2)

WDR5 (7)

By Research Areas:

Cancer (59)

Cardiovascular Disease (3)

Infection (13)

Inflammation/Immunology (8)

Metabolic Disease (5)

Neurological Disease (4)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Antibodies

GMP Molecules

Targets Recommended: Histone Methyltransferase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15593

Pinometostat 25+ Cited Publications EPZ-5676	Histone Methyltransferase	Cancer
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

HY-10442

3-Deazaneplanocin A Maximum Cited Publications 35 Publications Verification DZNep; 3-Deazaneplanocin	Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus	Infection Metabolic Disease Inflammation/Immunology Cancer
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .

HY-134124

*Glutathione ethyl* ester**	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-154812

Gintemetostat KTX-1001	Histone Methyltransferase CD44	Cancer
Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC₅₀ values ranging 0.460-2.17 nM and NSD2 SET domain IC₅₀ of 2.32 nM and K_d values ranging 6.3-70.4 nM .Gintemetostat reduces H₃K₃₆me₂ levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .

HY-112445

SGC3027 5+ Cited Publications	Histone Methyltransferase	Cancer
SGC3027 is a *histone methyltransferase* inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .

HY-N2019

Chaetocin 5+ Cited Publications	Histone Methyltransferase Bacterial Antibiotic	Infection Cancer
Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC₅₀ of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC₅₀ of 4 μM.

HY-12186

3-Deazaneplanocin A hydrochloride Maximum Cited Publications 35 Publications Verification DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride	Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus	Infection Inflammation/Immunology Cancer
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .

HY-100201

A-196 10+ Cited Publications	Histone Methyltransferase	Cancer
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC₅₀ values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .

HY-10587

BIX-01294 25+ Cited Publications	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-15273

UNC0638 10+ Cited Publications	VSV Histone Methyltransferase Autophagy Influenza Virus	Infection Cancer
UNC0638, a chemical probe, 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-12583

A-366 5+ Cited Publications	Histone Methyltransferase Epigenetic Reader Domain	Cancer
A-366, a chemical probe, 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-12220

MM-102 4 Publications Verification HMTase Inhibitor IX	WDR5 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-P10272

Rusfertide PTG-300	Ferroportin	Others
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .

HY-A0248A

Polymyxin B1 1 Publications Verification	Bacterial	Infection
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-13808

UNC 0631 5 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-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-16705

BRD4770 5 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-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-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-141429A

AS-99 TFA 2 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

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-148458

EZH2-IN-14	Histone Methyltransferase	Cancer
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .

HY-P1108A

Astressin 2B TFA 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-P1108

Astressin 2B 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-13808R

UNC 0631 (Standard)	Reference Standards Histone Methyltransferase	Cancer
UNC 0631 (Standard) is the analytical standard of UNC 0631. This product is intended for research and analytical applications. 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-108239

BIX-01294 trihydrochloride 25+ Cited Publications	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-114209

MRK-740 2 Publications Verification	Histone Methyltransferase	Cancer
MRK-740, a chemical probe, 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-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-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-133121

WDR5-IN-1	Apoptosis WDR5	Cancer
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a K_d of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC₅₀ of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .

HY-141430

AS-85	Histone Methyltransferase	Cancer
AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC₅₀=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the K_d value of 0.78 μM .

HY-P10948A

CS-VIP 8 hydrochloride	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .

HY-153331

DDO-2213	WDR5	Cancer
DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC₅₀ of 29 nM and a K_d value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .

HY-P10143

MMP-2/MMP-9 Substrate Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt	MMP	Others
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .

HY-A0248AS

Polymyxin B1-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-172614

RK-0080552 RK-552	Histone Methyltransferase Apoptosis	Cancer
RK-0080552 (RK-552) is a NSD2 inhibitor with an IC₅₀ of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC₅₀: 1.2 μM) and SET7/9 (IC₅₀: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .

HY-141429

AS-99 free base 2 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-148817

WDR5-0102	WDR5	Cancer
WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer .

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. ssK36 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-P10563

Noraramtide BHV-1100	CD38	Cancer
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .

HY-122936

Tanshindiol C	Histone Methyltransferase Keap1-Nrf2 Sirtuin	Cardiovascular Disease Cancer
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-P10948

CS-VIP 8	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .

HY-P10463A

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

HY-P3066

SKF 100398 d(CH2)5Tyr(Et)VAVP	Vasopressin Receptor	Metabolic Disease
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .

HY-121493

TM2-115	Histone Methyltransferase Parasite	Infection
TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death .

HY-142093

NSD3-IN-1	Histone Methyltransferase	Cancer
NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC₅₀ value of 28.58 μM .

HY-119164

DC-S238	Histone Methyltransferase	Metabolic Disease Inflammation/Immunology Cancer
DC-S238 is an orally active and highly selective histone methyltransferase SET7 (SETD7) inhibitor (IC₅₀=4.88 μM). DC-S238 is promising for research of cancer, diabetes and inflammatory diseases .

HY-12186G

3-Deazaneplanocin A hydrochloride DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride	Histone Methyltransferase Orthopoxvirus	Infection Cancer
3-Deazaneplanocin A (DZNep) hydrochloride (GMP) is 3-Deazaneplanocin A hydrochloride (HY-12186) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor .

HY-141429C

AS-99	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-149463

EZH2-IN-16	Histone Methyltransferase	Cancer
EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC₅₀ of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI₅₀ of 0.2 μM .

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.

HY-L203

Methylation Compound Library

338 compounds

Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases. The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation.

MCE contains 338 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.

Cat. No.	Product Name	Target	Research Area

HY-134124

*Glutathione ethyl* ester**	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-P10272

Rusfertide PTG-300	Ferroportin	Others
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .

HY-A0248A

Polymyxin B1 1 Publications Verification	Bacterial	Infection
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-P1108A

Astressin 2B TFA 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-P1108

Astressin 2B 1 Publications Verification	CRFR	Neurological Disease Inflammation/Immunology
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .

HY-P10948A

CS-VIP 8 hydrochloride	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .

HY-P10143

MMP-2/MMP-9 Substrate Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt	MMP	Others
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .

HY-A0248AS

Polymyxin B1-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

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. ssK36 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-P10563

Noraramtide BHV-1100	CD38	Cancer
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .

HY-P10948

CS-VIP 8	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .

HY-P10463A

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

HY-P3066

SKF 100398 d(CH2)5Tyr(Et)VAVP	Vasopressin Receptor	Metabolic Disease
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .

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 .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-P10570

[Nle20] H4 peptide (16−23)	Histone Methyltransferase	Cancer
[Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 (K_d=0.14 μM), which inhibits SETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .

HY-P4756

*N-(2-Carbamoyl-ethyl)-Val-Leu-anilide*	Peptides	Others
N-(2-Carbamoyl-ethyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .

HY-P2592

Ro 23-7014	Cholecystokinin Receptor	Others
Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7) .

HY-125628

Kahalalide A	Endogenous Metabolite	Infection
Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA	Isotope-Labeled Compounds Bacterial	Infection
Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2019

Chaetocin 5+ Cited Publications	Infection Alkaloids Microorganisms Classification of Application Fields Disease Research Fields Alkaloid Dimers Source Classification	Histone Methyltransferase Bacterial Antibiotic
Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC₅₀ of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC₅₀ of 4 μM.

HY-A0248A

Polymyxin B1 1 Publications Verification	Infection Microorganisms Classification of Application Fields Antibiotics Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	Bacterial
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-A0248AS

Polymyxin B1-d7 TFA	Structural Classification Microorganisms Antibiotics Antibacterial Disease Research Other Antibiotics Source Classification	Isotope-Labeled Compounds Bacterial
Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-122936

Tanshindiol C	Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Histone Methyltransferase Keap1-Nrf2 Sirtuin
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA	Structural Classification Microorganisms Antibiotics Antibacterial Disease Research Other Antibiotics Source Classification	Isotope-Labeled Compounds Bacterial
Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Cat. No.	Product Name	Chemical Structure

HY-A0248AS

Polymyxin B1-d7 TFA

Polymyxin B1-d₇ TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

HY-A0248AS1

Polymyxin B1-D-Leu-d7 TFA

Polymyxin B1-D-Leu-d₇ TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Host:	Mouse (1) Rabbit (3)
Reactivity:	Human (4) Mouse (3)
Application:	IHC-P (3) IF-Tissue (1) WB (4) FC (1)
Isotype:	IgG (3)
Conjugation:	Non-conjugated (4)
Clonality:	Monoclonal (3) Recombinant (2)
Modification:	Unmodified (3)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P81657

	KMT4 Antibody (YA1402) DOT 1; DOT1L; KMT4; Histone methyltransferase DOT1L; H3 lysine-79 specific	WB, IHC-P	Human, Mouse
	KMT4 Antibody (YA1402) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to KMT4.

HY-P81657A

	KMT4 Antibody (YA1402)(PBS only) DOT 1; DOT1L; KMT4; Histone methyltransferase DOT1L; H3 lysine-79 specific	WB, IHC-P	Human, Mouse
	KMT4 Antibody (YA1402) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to KMT4.

HY-P87161

	hSET1/SET1 Antibody (YA6854) Histone-lysine N-methyltransferase SETD1A antibody; hSET1A antibody; KMT2F antibody; Lysine N methyltransferase 2F antibody; Lysine N-methyltransferase 2F antibody; SET domain containing 1A antibody; SET domain containing protein 1A antibody; SET domain-containing protein 1A antibody; SET1 antibody; Set1 Ash2 histone methyltransferase complex subunit SET1 antibody; Histone-lysine N-methyltransferase SETD1A antibody; hSET1A antibody; KMT2F antibody; Lysine N methyltransferase 2F antibody; Lysine N-methyltransferase 2F antibody; SET domain containing 1A antibody; SET domain containing protein 1A antibody; SET domain-containing protein 1A antibody; SET1 antibody; Set1 Ash2 histone methyltransferase complex subunit SET1 antibody; Set1/Ash2 histone methyltransferase complex subunit SET1 antibody; SET1A antibody; SET1A_HUMAN antibody; SETD1A antibody;	WB, FC	Human
	hSET1/SET1 Antibody (YA6854) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to hSET1/SET1.

HY-P85491

	SMYD2 Antibody Histone methyltransferase SMYD2; HSKM B; HSKM-B; HSKMB; KMT3C; Lysine N-methyltransferase 3C; MGC119305; N lysine methyltransferase SMYD2; N-lysine methyltransferase SMYD2; SET and MYND domain containing 2; SET and MYND domain containing protein 2; SET and MYND domain-containing protein 2; Smyd2; SMYD2_HUMAN; Zinc finger MYND domain containing 14; ZMYND14.	WB, IHC-P, IF-Tissue	Human, Mouse
	SMYD2 Antibody is a Rabbit-derived and non-conjugated polyclonal antibody, targeting to SMYD2.

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Targets Recommended: Histone Methyltransferase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12186G

3-Deazaneplanocin A hydrochloride DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride	Histone Methyltransferase Orthopoxvirus	Infection Cancer
3-Deazaneplanocin A (DZNep) hydrochloride (GMP) is 3-Deazaneplanocin A hydrochloride (HY-12186) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor .

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Histone+Methyltransferase

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