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Results for "

covalent inhibitor

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (276) Cardiovascular Disease (14) Endocrinology (3) Infection (86) Inflammation/Immunology (50) Metabolic Disease (19) Neurological Disease (25)
Click Chemistry:	Azide (2) Alkynes (7)

425

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

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 .

HY-144448

FAK-IN-2	FAK Apoptosis	Cancer
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC₅₀= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .

HY-143899

FBA-IN-1	Fungal	Infection
FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC₈₀ of 1 μg/mL .

HY-161354

*JAK3 covalent* inhibitor-2**	JAK Apoptosis	Inflammation/Immunology
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC₅₀=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .

HY-119935

*JAK3 covalent* inhibitor-1**	JAK	Inflammation/Immunology
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC₅₀ of 11 nM and shows 246-fold selectivity vs other JAKs .

HY-163267

ZNL0325	Others	Others
ZNL0325 is a covalent probe based on pyrazolopyrimidine. ZNL0325 features an acrylamide side chain at the C3 position, which is capable of forming covalent bonds with multiple kinases that possess a cysteine at the αD-1 position, including BTK, EGFR, BLK, and JAK3. ZNL0325 can be used in the research of creating structurally distinct covalent kinase inhibitors .

HY-143474

POP-IN-3	Prolyl Endopeptidase (PREP)	Neurological Disease Cancer
Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a K_i of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer .

HY-143475

POP-IN-2	Prolyl Endopeptidase (PREP)	Neurological Disease Cancer
POP-IN-2 (Compound 7k) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a K_i of 6 nM. POP-IN-2 can be used for studying neurodegenerative diseases and cancer .

HY-157778

MK-7845	SARS-CoV	Infection
MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC₅₀ of 8.7 nM .

HY-150927

G12Si-2	Ras	Cancer
G12Si-2, an analog of G12Si-1 (HY-150926), is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12S mutant of K-Ras .

HY-156285

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 .

HY-154854

BBDDL2059	Histone Methyltransferase	Cancer
BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC₅₀ of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .

HY-161066

KRAS G13D-IN-1	Ras	Cancer
KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS ^G13D (IC₅₀: 0.41 nM). The selectivity for KRAS ^G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS ^G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .

HY-115902

FGFR4-IN-7	FGFR Apoptosis	Cancer
FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC₅₀ value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC) .

HY-161568

TEAD-IN-10	YAP	Cancer
TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC₅₀=14 nM), TEAD2 (IC₅₀=179 nM) and TEAD3 (IC₅₀=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research .

HY-144612

NS2B/NS3-IN-2	Flavivirus Dengue virus Virus Protease	Infection
NS2B/NS3-IN-2 is a potent dengue virus (DENV) NS2B/NS3 covalent inhibitor with an IC₅₀ of 6.0 nM and K_i of 0.66 µM. NS2B/NS3-IN-2 shows no cytotoxicity and markedly increases the cell survival rate .

HY-150510

MS8511	Histone Methyltransferase	Neurological Disease Cancer
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC₅₀ values of 100 nM (G9a) and 140 nM (GLP), and K_d values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .

HY-150022

GRK5-IN-4 CCG-265328	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research . GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-161569

TEAD-IN-11	YAP	Cancer
TEAD-IN-11 (compound 38) has a good inhibitory effect on TEAD1 (IC₅₀=8.7 nM), TEAD2 (IC₅₀=3.4 nM), TEAD3 (IC₅₀=5.6 nnM). TEAD-IN-11 has good selective activity against TEAD1-3 as a covalent inhibitor. TEAD-IN-11 can be used for cancer research .

HY-163527

FGFR-IN-13	FGFR	Cancer
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC₅₀=0.20±0.02 nM) and FGFR4(IC₅₀=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .

HY-122872

MKK7-COV-9	p38 MAPK	Cancer
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC₅₀ of 4.98 μM .

HY-143881

FGFR4-IN-6	FGFR	Cancer
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC₅₀ value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-161912

5TTU	JAK	Others
5TTU is a covalent JAK3 inhibitor. 5TTU not only forms a covalent bond with CYS909 but also establishes a hydrogen bond with the NH group of CYS909 .

HY-139878

MLKL-IN-1	Mixed Lineage Kinase	Inflammation/Immunology
MLKL-IN-1 is a covalent MLKL inhibitor with a K_D of 50 μM.

HY-123564

Mcl1-IN-7	Others	Others
Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.

HY-139881

BTK inhibitor 19	Btk	Cancer
BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC₅₀ = 2.7 nM).

HY-10544

Tegobuvir 4 Publications Verification GS 333126; GS-9190	HCV	Infection
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.

HY-10836

Cruzain-IN-1	Parasite	Others
Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC₅₀ of 10 nM.

HY-108691

PF-06465469	Itk	Cancer
PF-06465469 is a covalent inhibitor of ITK with an IC₅₀ of 2 nM .

HY-132879

TAK-020	Btk	Inflammation/Immunology
TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.

HY-W164560

RDR 03785	Macrophage migration inhibitory factor (MIF)	Inflammation/Immunology
RDR 03785 is a covalent MIF inhibitor with an IC₅₀ of 0.36 μM .

HY-130402B

Propamidine	Parasite	Infection
Propamidine is a covalent inhibitor of TMPRSS2 and has some antibacterial activity. .

HY-100944

Conduritol B epoxide 5+ Cited Publications	Glucosidase	Neurological Disease
Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.

HY-111512

PF-06795071	MAGL	Neurological Disease Inflammation/Immunology
PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC₅₀ of 3 nM .

HY-18081

PF 750	FAAH Autophagy	Metabolic Disease
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC₅₀s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile .

HY-139865

142I5	Apoptosis	Cancer
142I5 is a potent ML-IAP Lys-covalent inhibitor with an IC₅₀ value of 11 nM.

HY-116533

RMM-46	MAPKAPK2 (MK2)	Cancer
RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .

HY-123134

FIIN-4	Others	Cancer
FIIN-4 is a small molecule cysteine-targeting covalent kinase inhibitor (CKI) .

HY-18953

mTOR inhibitor-23	mTOR	Cancer
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .

HY-19564

JX06 1 Publications Verification	PDHK Apoptosis	Cancer
JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC₅₀s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity .

HY-52101A

FMK 3 Publications Verification	Ribosomal S6 Kinase (RSK)	Cancer
FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.

HY-112247

SR 16832	PPAR	Metabolic Disease
SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .

HY-149818

8BTC	Wnt	Cancer
8BTC (compound 4w) is a potent covalent Notum inhibitor with IC₅₀ of 2.5 nM .

HY-148535

Calpain Inhibitor XI	Proteasome	Neurological Disease
Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders .

HY-130149

Adagrasib 25+ Cited Publications MRTX849	Ras	Cancer
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .

HY-157145

SARS-CoV-2-IN-69	SARS-CoV	Infection
SARS-CoV-2-IN-69 (Compound 7E) is a non-covalent SARS-CoV-2 inhibitor with an EC₅₀ value of 7.4 μM. SARS-CoV-2-IN-69 is a potent inhibitor of SARS-CoV-2 main protease (M ^pro) and a non-covalent inhibitor of papain (PL ^pro) .

HY-101790

ZM223	NEDD8-activating Enzyme	Cancer
ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active .

HY-152248

ARS-2102	Ras	Cancer
ARS-2102 is a potent covalent KRAS G12C inhibitor for use in cancer research .

HY-158153

EGFR-IN-108	EGFR	Cancer
EGFR-IN-108 (Compound 12) is a selective and covalent EGFR inhibitor (pIC₅₀: 9.4) .

HY-U00279

Nitracrine	DNA/RNA Synthesis	Cancer
Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine has cytotoxicity towards most cells .

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus

3,023 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 3,023 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

HY-L036

Covalent Screening Library

1,710 compounds

MCE covalent inhibitor library contains 1,710 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L153

Cysteine Targeted Covalent Library

4,812 compounds

Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.

To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 4,812 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.

HY-L154

Cysteine Targeted Covalent Fragment Library

3,358 compounds

To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,358 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.

HY-L908

Lead-like Covalent Screening Library

500 compounds

MCE Lead-like Covalent Screening Library offers a valuable resource of 500 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.

HY-L909

Covalent Fragment Library

8,900 compounds

Covalent ligands rely on reactive groups (“warheads”), and new warheads are key to expanding the scope of covalent modalities. Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 8,900 fragment molecules with covalent modification potential, which can target various reactive amino acid residues and can be used for fragment-based covalent drug discovery.

HY-L0118V

Asinex Covalent Inhibitors Library	942 compounds
A unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target.

Cat. No.	Product Name	Type

HY-163624

Bfl-1-IN-2	Biochemical Assay Reagents
Bfl-1-IN-2 (Compound 13) is a reversible and covalent inhibitor of Bfl-1 (IC₅₀: 4.3 μM). Bfl-1-IN-2 acts by binding to Cys55 of Bfl-1 .

HY-141572

1,2-Dioleoyl-sn-glycerol

sn-1,2-Dioleoylglycerol

Drug Delivery

ALN29882 is a glycerolipid located on the plasma membrane. It consists of two fatty acid chains covalently linked to a single glycerol molecule by means of an ester bond. 18:1 DG has been used as a source of diacylglycerol in the diacylglycerol O-acyltransferase 1 (DGAT1) assay. It is also used as a substrate in the DGAT-1 enzyme assay to evaluate compounds as potential inhibitors of DGAT-1. Suitable for lipoprotein overlay screening assays with the recombinant protein His-AtROP6.

HY-W127409

1,2-Dimyristoyl-rac-glycerol

Drug Delivery

1,2-Dimyristoyl-rac-glycerol (C14:0) is a carboxylic acid ester, glycerolipid and diglyceride with an additional myristoyl group that facilitates interactions between proteins and lipids. Can be used as detergent or reagent. It plays a role in cell biology experiments involving the metabolism and metabolic pathways of glycerolipids. As a diglyceride, this substance consists of two fatty acid chains covalently bonded in the 1,2-form to a glycerol molecule. The diglyceride (DAG) study investigated the process by which DAG is depleted to inhibit fat accumulation. Reagent grade, for research use only.

Cat. No.	Product Name	Target	Research Area

HY-164725

FAPI-mFS	FAP	Cancer
FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu .

HY-P10428

E6AP-mimicking peptide	HPV	Infection
E6AP-mimicking peptide (compound 13) is a high-affinity, selective, irreversible and potent peptide-based covalent HPV16 E6 inhibitor targeting the 16E6 oncoprotein using a cysteine-reactive acrylamide warhead. E6AP-mimicking peptide has a K_i of 17 nM. E6AP-mimicking peptide targets all residues appearing in the binding pocket of E6 to disrupt the binding interface of 16E6 and E6AP. E6AP-mimicking peptide selectively binds and crosslinks to MBP-16E6 in PBS or a protein mixture .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3417

Kongensin A 1 Publications Verification	Classification of Application Fields Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields Croton kongensis Gagnep.	HSP RIP kinase Apoptosis Necroptosis
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications .

HY-N0191

Andrographolide Maximum Cited Publications 17 Publications Verification Andrographis	Infection Structural Classification Andrographis paniculata (Burm. F.) Nees Acanthaceae Classification of Application Fields 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.

HY-N5024

Gambogenic acid 1 Publications Verification	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Guttiferae Phenols Polyphenols Plants Garcinia hanburyi Hook. f. Disease Research Fields Cancer	Histone Methyltransferase
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .

HY-13821

Epoxomicin 10+ Cited Publications BU-4061T	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Inflammation/Immunology Disease Research Fields	Proteasome Apoptosis
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .

HY-113466

4-Hydroxynonenal 5+ Cited Publications 4-HNE	Structural Classification Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Disease markers Nervous System Disorder Endogenous metabolite Disease Research Fields Cancer	Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria .

HY-125826

Heptasaccharide Glc4Xyl3	Structural Classification Polysaccharides Microorganisms Classification of Application Fields Source classification Metabolic Disease Disease Research Fields Saccharides	Others
Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature[1].

HY-N12776

Illudalic acid	Structural Classification Microorganisms Terpenoids Sesquiterpenes Source classification	Phosphatase
Illudalic acid is a potent and selective Leukocyte antigen-related (LAR) phosphatase inhibitor with an IC₅₀ value of 1.30 µM. Illudalic acid inhibits LAR phosphatase through covalent ligation to the catalytic cysteine residue .

HY-121360

Cylindrospermopsin	Microorganisms Source classification	DNA/RNA Synthesis
Cylindrospermopsin is a cyanotoxin produced by a variety of freshwater cyanobacteria. It is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA .

HY-N8306

Isojacareubin	Structural Classification Flavonoids Flavones Source classification Guttiferae Plants Hypericum japonicum Thunb. ex Murray	Bacterial PKC Apoptosis SARS-CoV
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis .

HY-N0191R

Andrographolide (Standard)	Structural Classification Andrographis paniculata (Burm. F.) Nees Acanthaceae Terpenoids Source classification Diterpenoids Plants	NF-κB SARS-CoV Influenza Virus Autophagy Parasite
Andrographolide (Standard) is the analytical standard of Andrographolide. This product is intended for research and analytical applications. 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.

Cat. No.	Product Name	Chemical Structure

HY-15772S1

Osimertinib-13C,d3
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-15772S

Osimertinib-d6
Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

HY-113466S

4-Hydroxynonenal-d3

4-Hydroxynonenal-d₃ is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria[1][2][3].

HY-16293S

Lurbinectedin-d3
Lurbinectedin-d₃ is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].

HY-114277S

Sotorasib-d7
Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .

HY-114436S

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-W757743

Acalabrutinib-d3
Acalabrutinib-d₃ (ACP-196-d₃) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).

HY-B0712S1

Ceftriaxone-13C2,d3 triethylammonium salt

Ceftriaxone- ¹³C₂,d₃ triethylammonium salt is ¹³C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .

Cat. No.	Product Name		Classification

HY-148254

8RK64		Azide
8RK64 is a covalent UCHL1 inhibitor (IC₅₀: 0.32 μM) . 8RK64 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-100433

PACMA 31		Alkynes
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC₅₀ of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-117570

KSC-34		Alkynes
KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC₅₀ of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-161407

AURKA-IN-1		Alkynes
AURKA-IN-1 (compound 9) is an cell-active covalent AURKA inhibitor. AURKA-IN-1 is a lysine-reactive activity probe .

HY-158007

(RS)-G12Di-1		Alkynes
(RS)-G12Di-1 is a selective, covalent inhibitor of K-Ras-G12D .

HY-126943

SAHA-BPyne		Alkynes
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC₅₀ of less than 5 μM .

HY-125384

ARN14686		Alkynes
ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC₅₀=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .

HY-115715A

EN219-alkyne		Alkynes
EN219-alkyne is an alkyne-functionalized EN219 probe. EN219 (HY-P0287A) is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC₅₀ of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination . EN219-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-134318B

8-Azido-ADP disodium		Azide
8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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