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trimethylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Bacterial (1) CD38 (1) CFTR (2) Cholecystokinin Receptor (1) Deubiquitinase (1) Endogenous Metabolite (1) Ferroportin (1) Histone Acetyltransferase (1) Histone Demethylase (1) Histone Methyltransferase (7) MDM-2/p53 (1) MMP (1) NF-κB (1) Vasopressin Receptor (1) Virus Protease (1) WDR5 (1)
By Research Areas:	Cancer (12) Infection (3) Inflammation/Immunology (2) Metabolic Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114209

MRK-740 1 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-P2257

H3K4(Me3) (1-20)	Histone Demethylase	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-18935

CBL0137 Maximum Cited Publications 9 Publications Verification Curaxin 137; CBL-C137	Histone Acetyltransferase MDM-2/p53 NF-κB	Cancer
CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis .

HY-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-132922

EEDi-5273 APG-5918	Histone Methyltransferase	Cancer
EEDi-5273 is a potent and orally active embryonic ectoderm development (EED) inhibitor with an IC₅₀ of 0.2 nM. EEDi-5273 can inhibit the polycomb repressive complex 2 (PRC2) activity and block trimethylation of histone H3 lysine 27. EEDi-5273 can be used for the research of cancer, such as ovarian cancer .

HY-16993

OICR-9429 Maximum Cited Publications 9 Publications Verification	Apoptosis WDR5	Cancer
OICR-9429, a chemical probe, 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-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 (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .

HY-172824

MS7131	Deubiquitinase	Cancer
MS7131 is a USP1-recruiting DUBTACs. MS7131 effectively reduces histone H3 lysine 27 trimethylation and significantly suppresses the proliferation and clonogenicity of cancer cells .

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-174372

EZH2-IN-23	Histone Methyltransferase	Cancer
EZH2-IN-23 (Compound 25) is an EZH2 inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex (EZH2, EED, SUZ12, AEBP2, RbAp48) with a biochemical IC₅₀ of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC₅₀ of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability.

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-P1108A

Astressin 2B TFA	CFTR	Others
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .

HY-P1108

Astressin 2B	CFTR	Others
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

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-P4521

*Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt*	MMP	Others
Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt is a MMP12 substrate, and can be used to detect MMP12 enzyme activity .

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-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-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-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 .

Cat. No.	Product Name	Target	Research Area

HY-P2257

H3K4(Me3) (1-20)	Histone Demethylase	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-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-P1108A

Astressin 2B TFA	CFTR	Others
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .

HY-P1108

Astressin 2B	CFTR	Others
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .

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-P10111

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 .

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-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-P4521

*Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt*	MMP	Others
Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt is a MMP12 substrate, and can be used to detect MMP12 enzyme activity .

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-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-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 .

Polymyxin B1 1 Publications Verification	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	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 .

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trimethylation

Inhibitors & Agonists

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