covalent modification

By Targets:	Autophagy (2) Btk (1) DNA Alkylator/Crosslinker (1) DNA Methyltransferase (1) EGFR (1) Influenza Virus (1) Isocitrate Dehydrogenase (IDH) (1) MDM-2/p53 (1) Microtubule/Tubulin (1) NF-κB (1) Parasite (1) SARS-CoV (1) TRP Channel (1)
By Research Areas:	Cancer (6) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-119390

AA-CW236

DNA Methyltransferase Cancer

AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .

AA-CW236	DNA Methyltransferase	Cancer
AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .

HY-121539

Supercinnamaldehyde	TRP Channel	Neurological Disease
Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC₅₀ value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines .

HY-128661

IDH1 Inhibitor 2	Isocitrate Dehydrogenase (IDH)	Metabolic Disease
IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC₅₀ of 110 nM .

HY-13943

CNX-774 1 Publications Verification	Btk	Cancer
CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC₅₀ of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification .

HY-U00447

PK11000	MDM-2/p53 DNA Alkylator/Crosslinker	Cancer
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .

HY-16909

Leptomycin B 5 Publications Verification CI 940; LMB
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .

HY-137028

2′-Thioadenosine PD157432	EGFR	Cancer
2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC₅₀ of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site .

HY-N0191

Andrographolide Maximum Cited Publications 16 Publications Verification Andrographis	NF-κB SARS-CoV Influenza Virus Autophagy Parasite	Infection Inflammation/Immunology Cancer
Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

HY-128892

EN6 2 Publications Verification	Autophagy	Neurological Disease
EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner .

HY-163105

Tubulin/NEDDylation-IN-1	Microtubule/Tubulin	Cancer
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC₅₀ for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library	614 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 614 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.

Histone Modification Research Compound Library

614 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 614 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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0191

Andrographolide 15+ Cited Publications Andrographis	Infection Andrographis paniculata (Burm. F.) Nees Classification of Application Fields Acanthaceae Terpenoids Source classification Diterpenoids Plants Inflammation/Immunology Disease Research Fields	NF-κB SARS-CoV Influenza Virus Autophagy Parasite
Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

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covalent modification

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