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Irreversible+Inhibitors

" in MedChemExpress (MCE) Product Catalog:

標的別:	17β-HSD (1) Acyltransferase (1) Adenosine Deaminase (2) Akt (3) Antibiotic (16) Apoptosis (32) Autophagy (12) Bacterial (19) Biochemical Assay Reagents (2) BMX Kinase (2) Btk (4) c-Met/HGFR (2) Calcium Channel (1) Carnitine Palmitoyltransferase (CPT) (4) Caspase (9) Cathepsin (12) CD38 (1) Ceramidase (1) Cholinesterase (ChE) (4) COX (8) Cyclic GMP-AMP Synthase (1) Cytochrome P450 (10) DAGL (2) Dengue Virus (3) Deubiquitinase (1) Dipeptidyl Peptidase (1) DNA/RNA Synthesis (3) Drug Isomer (1) Drug Metabolite (3) E1/E2/E3 Enzyme (1) EGFR (15) Endogenous Metabolite (3) Enterovirus (3) Environmental Pollutants (3) Epoxide Hydrolase (1) Factor Xa (1) Fatty Acid Synthase (FASN) (3) Ferroptosis (3) FGFR (3) Filovirus (2) Flavivirus (3) Fungal (1) GABA Receptor (3) Glutaminase (3) Glutathione Peroxidase (2) Glutathione S-transferase (1) Histone Demethylase (7) Histone Methyltransferase (2) HIV (2) HSV (3) IKK (1) Indoleamine 2,3-Dioxygenase (IDO) (1) Influenza Virus (5) Insecticide (3) Isotope-Labeled Compounds (14) JNK (1) Legumain (1) Ligands for Target Protein for PROTAC (1) LPL Receptor (1) Macrophage migration inhibitory factor (MIF) (1) MAGL (4) MALT1 (1) MAPKAPK2 (MK2) (1) MEK (1) MetAP (3) Mitochondrial Metabolism (1) Mitophagy (9) Monoamine Oxidase (10) NF-κB (10) Nucleoside Antimetabolite/Analog (3) OAT (1) Orthopoxvirus (1) P2Y Receptor (3) p38 MAPK (11) Parasite (11) PARP (2) PD-1/PD-L1 (1) Phosphatase (2) Phosphodiesterase (PDE) (1) Phospholipase (3) PI3K (1) Prostaglandin Receptor (4) Proteasome (3) Protein Arginine Deiminase (1) Proton Pump (6) Ras (6) Reactive Oxygen Species (ROS) (1) Reference Standards (30) SARS-CoV (7) Ser/Thr Protease (3) Src (3) Steroid Sulfatase (4) STING (1) Thrombin (1) TOPK (5) Topoisomerase (1) Transmembrane Glycoprotein (1) VEGFR (1) Virus Protease (12)
研究分野別:	Cancer (111) Cardiovascular Disease (17) Endocrinology (1) Infection (51) Inflammation/Immunology (42) Metabolic Disease (27) Neurological Disease (35)
クリックケミストリー:	Alkynes (7)

202

阻害剤およびアゴニスト

スクリーニングライブラリ

ペプチド

天然物

同位体標識化合物

クリックケミストリー

製品番号	製品名	Target	研究分野	構造式

HY-50202

Etomoxir 125+ Cited Publications (R)-(+)-Etomoxir	Carnitine Palmitoyltransferase (CPT) Apoptosis	Metabolic Disease Cancer
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

HY-15282

E-64 20+ Cited Publications Proteinase inhibitor E 64	Cathepsin Autophagy Bacterial	Inflammation/Immunology Cancer
E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

HY-B0744

Eflornithine 20+ Cited Publications DFMO; MDL71782; RMI71782; α-difluoromethylornithine	Parasite	Infection Cancer
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

HY-112847A

Sulfosuccinimidyl oleate sodium 35+ Cited Publications Sulfo-N-succinimidyl oleate sodium	Mitophagy	Inflammation/Immunology
Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect .

HY-106376A

L-Buthionine-(S,R)-sulfoximine 15+ Cited Publications L-Buthionine sulfoximine; L-BSO	Ferroptosis	Cancer
L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC₅₀ value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.

HY-12821

AEBSF hydrochloride 15+ Cited Publications	Thrombin Influenza Virus Ser/Thr Protease	Others
AEBSF hydrochloride is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.

HY-103389

1-Aminobenzotriazole 5+ Cited Publications ABT; 3-Aminobenzotriazole	Cytochrome P450	Cancer
1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).

HY-B0744B

Eflornithine hydrochloride hydrate 20+ Cited Publications DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate	Parasite	Cancer
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women .

HY-B0218

Orlistat 30+ Cited Publications Tetrahydrolipstatin; Ro-18-0647	Fatty Acid Synthase (FASN) Apoptosis	Metabolic Disease Cancer
Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity . Anti-atherosclerotic effect .

HY-50202A

Etomoxir sodium salt 125+ Cited Publications (R)-(+)-Etomoxir sodium salt	Carnitine Palmitoyltransferase (CPT) Apoptosis	Metabolic Disease Cancer
Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig .

HY-A0006

Pentostatin 5+ Cited Publications CI-825; Deoxycoformycin	Adenosine Deaminase Antibiotic	Cancer
Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with K_i of 2.5 pM.

HY-75054

Abiraterone acetate 20+ Cited Publications CB7630	Cytochrome P450	Cancer
Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

HY-13272

Dacomitinib 25+ Cited Publications PF-00299804; PF-299804	EGFR Apoptosis	Cancer
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .

HY-14199

Selegiline hydrochloride 5+ Cited Publications Deprenyl hydrochloride; (-)-Selegiline hydrochloride; (-)-Deprenyl hydrochloride	Monoamine Oxidase	Neurological Disease
Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline hydrochloride can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .

HY-103334

MAFP 5 Publications Verification Methyl Arachidonyl Fluorophosphonate	Phospholipase	Cardiovascular Disease Neurological Disease Metabolic Disease
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

HY-110063

4-IPP 10+ Cited Publications 4-Iodo-6-phenylpyrimidine	Macrophage migration inhibitory factor (MIF)	Metabolic Disease
4-IPP (4-Iodo-6-phenylpyrimidine) is a specific suicide substrate and irreversible inhibitor of macrophage migration inhibitory factor (MIF) .

HY-18632

GSK2879552 15+ Cited Publications	Histone Demethylase	Cancer
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity .

HY-125006

TRi-1 5 Publications Verification	JNK p38 MAPK	Cancer
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC₅₀ of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy .

HY-P1010

Z-LEHD-FMK 10+ Cited Publications	Caspase Apoptosis	Neurological Disease Cancer
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .

HY-B0744A

Eflornithine hydrochloride 20+ Cited Publications DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride	Parasite	Infection Cancer
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

HY-13734

PX-12 10+ Cited Publications IV-2	Apoptosis	Cancer
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC₅₀ values of 1.9 and 2.9 μM, respectively.

HY-111341

AZD5904 10+ Cited Publications	Glutathione Peroxidase	Neurological Disease
AZD5904 is a selective and irreversible inhibitor of human Myeloperoxidase (MPO) with an IC₅₀ of 140 nM and has similar potency in mouse and rat.

HY-18632A

GSK2879552 dihydrochloride 15+ Cited Publications	Histone Demethylase	Cancer
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity .

HY-32718

Pelitinib 5+ Cited Publications EKB-569; WAY-EKB 569	EGFR Src	Cancer
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC₅₀ of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC₅₀s of 282, 800, and 1255 nM, respectively.

HY-106014

Tezacitabine	DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis	Cancer
Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment .

HY-118284

Vicagrel 1 Publications Verification	P2Y Receptor	Cardiovascular Disease
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease .

HY-12015

Iniparib 5+ Cited Publications BSI-201; NSC-746045; IND-71677	PARP Influenza Virus	Cancer
Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.

HY-18602

FIIN-2	FGFR	Cancer
FIIN-2 is an irreversible inhibitor of FGFR with an IC₅₀ of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

HY-N6781

Ophiobolin A	Phosphodiesterase (PDE)	Infection Cancer
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC₅₀ value of 9 μM. Ophiobolin A antimicrobial and anticancer activity .

HY-114304

COH000 2 Publications Verification	E1/E2/E3 Enzyme	Cancer
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC₅₀ of 0.2 μM for SUMOylation in vitro .

HY-112161

Branebrutinib 3 Publications Verification BMS-986195	Btk	Cancer
Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC₅₀ of 0.1 nM . Branebrutinib 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-16677A

Mofegiline hydrochloride MDL72974A	Monoamine Oxidase	Neurological Disease
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC₅₀s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) .

HY-14198

Selegiline Deprenyl; (-)-Selegiline; (-)-Deprenyl	Monoamine Oxidase	Neurological Disease
Selegiline (Deprenyl) is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .

HY-13929

Isocarboxazid 2 Publications Verification	Monoamine Oxidase	Neurological Disease
Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC₅₀ of 4.8 μM for rat brain monoamine oxidase in vitro .

HY-102087

JPM-OEt 3 Publications Verification	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .

HY-N0688

Linderane	Cytochrome P450	Inflammation/Immunology
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .

HY-112205A

RR-11a analog 5+ Cited Publications	Parasite Legumain	Infection
RR-11a analog is a potent and irreversible inhibitor of Schistosoma mansoni legumain, with an IC₅₀ of 31 nM. RR-11a analog is an aza-Asn derivative and aza-peptide Michael acceptor .

HY-154021A

5-Fluoromethylornithine dihydrochloride 5-FMOrn dihydrochloride	OAT	Metabolic Disease
5-Fluoromethylornithine (5-FMOrn) dihydrochloride is a specific irreversible inhibitor of L-ornithine:2-oxoacid aminotransferase (OAT). 5-Fluoromethylornithine dihydrochloride can be used in the study of gyrate atrophy of choroid and retina .

HY-W009706

Alclofenac Allopydin; W-7320	Prostaglandin Receptor	Neurological Disease Inflammation/Immunology
Alclofenac (Allopydin) is an orally active prostaglandin synthase inhibitor with anti-inflammatory, analgesic and antipyretic activities. Alclofenac irreversibly inhibits platelet aggregation. Alclofenac can be used in research related to rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, low back pain and sciatica .

HY-101457

JZP-430	MAGL	Metabolic Disease
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC₅₀ of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL) .

HY-118969

BMS-262084	Factor Xa Ser/Thr Protease	Cardiovascular Disease
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC₅₀ of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC₅₀=5 nM). BMS-262084 exhibits antithrombotic effects .

HY-122635A

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

HY-112318A

GSK-2793660	Cathepsin	Inflammation/Immunology
GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis .

HY-13731

PPI-2458	MetAP	Inflammation/Immunology Cancer
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research .

HY-B0218R

Orlistat (Standard) 30+ Cited Publications Tetrahydrolipstatin (Standard); Ro-18-0647 (Standard)	Reference Standards Fatty Acid Synthase (FASN) Apoptosis	Metabolic Disease Cancer
Orlistat (Standard) is the analytical standard of Orlistat. This product is intended for research and analytical applications. Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity . Anti-atherosclerotic effect .

HY-130430

Neplanocin A (-)-Neplanocin A	Antibiotic Orthopoxvirus	Infection Cancer
Neplanocin A ((-)-Neplanocin A) is an antitumor antibiotic with significant antitumor activity against murine L1210 leukemia. Neplanocin A is also an irreversible inhibitor of AdoHcy hydrolase (K_i=8.39 nM). Neplanocin A also has antiviral activity and is effective against vaccinia virus. Neplanocin A is obtained from Ampulariella regularis .

HY-123669A

trans-R-138727	P2Y Receptor	Cardiovascular Disease
Trans-R-138727 is the trans isomer of R-138727 (HY-123669). R-138727 is the active metabolite of the antiplatelet agent Prasugrel (HY-15284). R-138727 is an irreversible inhibitor for the platelet receptor P2Y12, and inhibits ADP-induced platelet activation and aggregation .

HY-W796158

Z-DEVD-CMK	Cathepsin	Inflammation/Immunology
Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro .

HY-136562

N-Arachidonyl maleimide	MAGL	Metabolic Disease
N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC₅₀ value of 140 nM .

HY-15377

DL-Gabaculine hydrochloride	GABA Receptor	Neurological Disease
DL-Gabaculine hydrochloride is a neurotoxin that irreversibly inhibits bacterial pyridoxal phosphate linked γ-aminobutyric acid-α-ketoglutaric acid transaminase with a K_i of 2.86 μM .

製品番号	製品名

HY-L036

Covalent Screening Library

1,546 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 1,546 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-L908

Lead-like Covalent Screening Library

1,248 compounds

MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 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-L036P

Covalent Screening Library Plus

5,994 compounds

MCE covalent inhibitor library contains 5,994 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.

製品番号	製品名	Category	Target	構造式

HY-W016420

Fosfomycin sodium 10+ Cited Publications MK-0955 sodium	Infection Structural Classification 天然物 Microorganisms Classification of Application Fields Disease Research Fields Source Classification	Bacterial Antibiotic
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .

HY-N6781

Ophiobolin A	Infection Microorganisms Classification of Application Fields Terpenoids Sesquiterpenes Disease Research Fields Source Classification	Phosphodiesterase (PDE)
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC₅₀ value of 9 μM. Ophiobolin A antimicrobial and anticancer activity .

HY-129476

L-Canaline	Infection other families Classification of Application Fields Amino acids Plants Endogenous metabolite Disease Research Fields Source Classification	Parasite Endogenous Metabolite
L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite *Plasmodium falciparum* with an IC₅₀ of 297 nM. L-Canaline has anticancer and antiproliferative effects .

HY-N0688

Linderane	Classification of Application Fields Terpenoids Sesquiterpenes Plants Lauraceae Lindera aggregata (Sims) Kosterm. Inflammation/Immunology Disease Research Fields Source Classification	Cytochrome P450
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .

HY-N4202

Dihydrorotenone	Structural Classification Erycibe ferruginea C. Y. Wu Flavonoids Neurological Disease Classification of Application Fields Isoflavanones Plants Convolvulaceae Disease Research Fields Biological Pesticide Research Source Classification Agricultural Research	Environmental Pollutants Insecticide Apoptosis p38 MAPK
Dihydrorotenone is an insecticide and irreversible inhibitor of mitochondrial complex I. Dihydrorotenone may induce Parkinson's disease. Dihydrorotenone induces apoptosis in human plasma cells by triggering endoplasmic reticulum stress and activating the p38 signaling pathway. The oral LD₅₀ of dihydrorotenone in rats is approximately 2.5 g/kg. Dihydrorotenone exhibits insecticide activity and cytotoxicity to plasma cells. Dihydrorotenone can be used to establish animal models of Parkinson's disease, safety assessment of natural pesticides, and potential cancer chemoprevention studies .

HY-130430

Neplanocin A (-)-Neplanocin A	天然物 Microorganisms Source Classification	Antibiotic Orthopoxvirus
Neplanocin A ((-)-Neplanocin A) is an antitumor antibiotic with significant antitumor activity against murine L1210 leukemia. Neplanocin A is also an irreversible inhibitor of AdoHcy hydrolase (K_i=8.39 nM). Neplanocin A also has antiviral activity and is effective against vaccinia virus. Neplanocin A is obtained from Ampulariella regularis .

HY-126765

Territrem B	Structural Classification 天然物 Marine natural products Marine microorganism Source Classification	Cholinesterase (ChE)
Territrem B is an irreversible inhibitor of Acetylcholinesterase (AChE) inhibitor. Territrem B is also a fungal meroterpenoid that can be isolated from Aspergillus terreus .

HY-N0688R

Linderane (Standard)	Terpenoids Sesquiterpenes Plants Lauraceae Lindera aggregata (Sims) Kosterm. Source Classification	Reference Standards Cytochrome P450
Linderane (Standard) is the analytical standard of Linderane. This product is intended for research and analytical applications. Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .

製品番号	製品名	構造式

HY-14654S1

Aspirin-d4

Aspirin-d₄ is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis .

HY-14654S

Aspirin-d3

Aspirin-d₃ is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis .

HY-114277S

Sotorasib-d7

Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

HY-B0218S

Orlistat-d3
Orlistat-d3 is a deuterated labeled Orlistat . Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect .

HY-B1075AS

(Rac)-Fosfomycin (benzylamine)-13C3

(Rac)-Fosfomycin (benzylamine)- ¹³C₃ is the ¹³C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .

HY-114277S2

Sotorasib-d3
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .

HY-75054S

Abiraterone acetate-d4
Abiraterone acetate-d₄ is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

HY-13272S2

Dacomitinib-d10 dihydrochloride
Dacomitinib-d₁₀ dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .

HY-13272S3

Dacomitinib-d10
Dacomitinib-d₁₀ is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .

HY-75054S1

Abiraterone acetate-d3
Abiraterone acetate-d₃ (CB7630-d₃) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598) .

HY-32718S

Pelitinib-d6
Pelitinib-d₆ (EKB-569-d₆) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC₅₀ of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC₅₀s of 282, 800, and 1255 nM, respectively .

HY-14199S

Selegiline-d5 hydrochloride

Selegiline-d₅ (hydrochloride) (Deprenyl-d₅ (hydrochloride)) is deuterium labeled Selegiline (hydrochloride). Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline hydrochloride can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .

HY-14198S

Selegiline-d5
Selegiline-d₅ (Deprenyl-d₅) is deuterium labeled Selegiline. Selegiline (Deprenyl) is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .

HY-106161S1

Rupintrivir-d7

Rupintrivir-d7 is a deuterated labeled Rupintrivir . Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC₅₀ of 0.023 μM. Rupintrivirvr shows immune-modulatory effect .

HY-W707656

Aspirin-d7

Aspirin-d₇ is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis .

HY-17447AS

(1S,2R)-Tranylcypromine-d5 hydrochloride

(1S,2R)-Tranylcypromine-d₅ (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride . Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC₅₀s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression .

HY-B1120S

Temephos-d12

Temephos-d₁₂ is the deuterium labeled Temephos. Temephos (Temefos) is an orally active, blood-brain barrier-permeable organophosphate insecticide and AChE inhibitor. By irreversibly inhibiting AChE to induce cholinergic overactivation, Temephos effectively blocks larval development of Aedes aegypti (yellow fever mosquito) and Aedes albopictus (Asian tiger mosquito), and is commonly used in studies related to Dengue Virus, Zika Virus and other relevant pathogens. Temephos exhibits genotoxicity and neurodevelopmental toxicity, and may also cause liver injury, reproductive system abnormalities and cholinergic poisoning symptoms in mammals. Temephos tends to accumulate in adipose tissues and aquatic organisms, and is excreted via feces after metabolism through oxidation and hydrolysis. Note that CYP-mediated metabolic detoxification may reduce the actual larvicidal efficacy of Temephos against some mosquito species. Temephos can be used in research related to dengue fever, Zika virus disease, chikungunya and dracunculiasis .

製品番号	製品名		Classification

HY-115673

LAS17 1 Publications Verification		Alkynes
LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC₅₀ of 0.5 μM . LAS17 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-10533

Eniluracil 1 Publications Verification 5-Ethynyluracil; GW776C85		Alkynes
Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil) . Eniluracil 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-19476

AG-7404		Alkynes
AG-7404 is an orally active, irreversible inhibitor of the picornavirus 3C protease. AG-7404 blocks the processing of viral polyproteins, thereby inhibiting viral replication. AG-7404 has synergistic antiviral activity with capsid inhibitors such as V-073 (HY-104074) or BTA798 (HY-106254) and is effective against V-073-resistant variants. AG-7404 is used in the study of enterovirus infections such as poliovirus .

HY-131693A

γ-Acetylenic GABA hydrochloride GAG hydrochloride		Alkynes
γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA hydrochloride can increase the concentration of GABA in rat brain . γ-Acetylenic GABA (hydrochloride) 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-119532

Nordeprenyl Desmethylselegiline		Alkynes
Nordeprenyl is the metabolite of Deprenyl. Deprenyl is a potent, selective and irreversible inhibitor of MAO-B . Nordeprenyl 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-131693

γ-Acetylenic GABA GAG		Alkynes
γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain . γ-Acetylenic GABA 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-14198B

(±)-Selegiline hydrochloride (±)-Deprenyl hydrochloride		Alkynes
(±)-Selegiline (Deprenyl) hydrochloride is the racemic of Selegiline (HY-14198). Selegiline is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .

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