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Results for "

Irreversible

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) ADC Linker (2) Adenosine Deaminase (2) Adenosine Receptor (1) Adrenergic Receptor (6) Akt (3) Aldehyde Dehydrogenase (ALDH) (1) Amyloid-β (1) Antibiotic (20) Apoptosis (62) Arp2/3 Complex (1) Aurora Kinase (3) Autophagy (26) Bacterial (32) Bcl-2 Family (1) Bcr-Abl (1) Biochemical Assay Reagents (1) BMX Kinase (4) Btk (31) c-Met/HGFR (4) Calcium Channel (2) Cannabinoid Receptor (1) Caspase (17) Cathepsin (14) CCR (1) CDK (5) Cholinesterase (ChE) (4) COX (10) CRM1 (1) Cytochrome P450 (17) Dengue virus (1) Deubiquitinase (3) DNA Alkylator/Crosslinker (3) DNA Methyltransferase (2) DNA/RNA Synthesis (5) Drug Metabolite (7) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) EGFR (62) Elastase (2) Endogenous Metabolite (4) Enterovirus (1) Epigenetic Reader Domain (2) ERK (1) Estrogen Receptor/ERR (2) FAAH (7) Factor Xa (3) Fatty Acid Synthase (FASN) (3) Ferroptosis (2) FGFR (8) Filovirus (1) Flavivirus (2) FLT3 (1) Fluorescent Dye (3) Fungal (2) GABA Receptor (7) Glucosidase (1) Glutaminase (3) Glutathione Peroxidase (3) Glutathione S-transferase (2) Glyoxalase (GLO) (1) GlyT (1) GSK-3 (3) HDAC (2) Histamine Receptor (1) Histone Demethylase (16) Histone Methyltransferase (8) HIV (5) HSV (4) IKK (1) Indoleamine 2,3-Dioxygenase (IDO) (4) Influenza Virus (4) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (17) Itk (1) JAK (2) Legumain (1) Ligands for Target Protein for PROTAC (1) LPL Receptor (1) Macrophage migration inhibitory factor (MIF) (1) MAGL (7) MALT1 (4) MAP3K (1) MAPKAPK2 (MK2) (1) MEK (1) MetAP (1) Microtubule/Tubulin (1) Mitophagy (7) Monoamine Oxidase (27) NF-κB (5) NOD-like Receptor (NLR) (2) Notch (1) Nucleoside Antimetabolite/Analog (5) Organoid (1) Orthopoxvirus (5) P2X Receptor (1) P2Y Receptor (3) p38 MAPK (6) PAI-1 (1) Parasite (19) PARP (1) Phosphatase (5) Phosphodiesterase (PDE) (1) Phospholipase (6) PI3K (2) Polo-like Kinase (PLK) (1) Potassium Channel (2) PPAR (1) PROTACs (1) Proteasome (9) Proton Pump (8) Ras (9) Reactive Oxygen Species (3) Ribosomal S6 Kinase (RSK) (1) ROS Kinase (2) SARS-CoV (9) Ser/Thr Protease (5) Sigma Receptor (1) Sodium Channel (3) SphK (1) Src (2) SRPK (1) Steroid Sulfatase (6) Thrombin (4) Thymidylate Synthase (2) Toll-like Receptor (TLR) (1) TOPK (2) Topoisomerase (1) Tryptophan Hydroxylase (1) VEGFR (1) Virus Protease (10) Wnt (1) YAP (3)
By Research Areas:	Cancer (291) Cardiovascular Disease (25) Endocrinology (10) Infection (64) Inflammation/Immunology (71) Metabolic Disease (30) Neurological Disease (57)
Click Chemistry:	Labeling and Fluorescence Imaging (2) Azide (2) Alkynes (18)

475

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15813

FIIN-1 FGFR Irreversible inhibitor-1	FGFR	Cancer
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with K_ds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC₅₀s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively .

HY-115733

Cathepsin L-IN-2

(Rac)-Z-Phe-Phe-FMK
Cathepsin Cancer

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor .
HY-139384

FAAH inhibitor 2

FAAH Neurological Disease

FAAH inhibitor 2 (Compound 17b) is an irreversible fatty acid amide hydrolase (FAAH) inhibitor, with an IC₅₀ of 0.153 μM .
HY-145057

PP-biotin

Others Cancer

PP-biotin is an irreversible, biotin-labeled probe .
HY-137495

GGACK

PAI-1 Ser/Thr Protease Cancer

GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .

Cathepsin L-IN-2 (Rac)-Z-Phe-Phe-FMK	Cathepsin	Cancer
Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor .

FAAH inhibitor 2	FAAH	Neurological Disease
FAAH inhibitor 2 (Compound 17b) is an irreversible fatty acid amide hydrolase (FAAH) inhibitor, with an IC₅₀ of 0.153 μM .

PP-biotin	Others	Cancer
PP-biotin is an irreversible, biotin-labeled probe .

GGACK	PAI-1 Ser/Thr Protease	Cancer
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .

HY-W014134

p-APMSF hydrochloride p-Amidinophenylmethylsulfonylfluoride hydrochloride	Others	Others
p-APMSF is an irreversible inhibitor of serinase. p-APMSF has substrate specificity for positively charged side chains of amino acids, lysine, or arginine. p-APMSF can be used to study the irreversible inhibition of trypsin and thrombin .

HY-121558

JP104

FAAH Neurological Disease

JP104, a aryl carbamate, is an irreversible FAAH inhibitor with a pIC₅₀ of ~8 .

JP104	FAAH	Neurological Disease
JP104, a aryl carbamate, is an irreversible FAAH inhibitor with a pIC₅₀ of ~8 .

HY-15375

Allitinib AST-1306; ALS 1306	EGFR	Cancer
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity .

HY-13427

Allitinib tosylate AST-1306 (TsOH)	EGFR	Cancer
Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity

HY-B1368

Fenclonine 10+ Cited Publications 4-Chloro-DL-phenylalanine; PCPA; CP-10188	Tryptophan Hydroxylase	Neurological Disease Cancer
Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research .

HY-136605

DGY-06-116 1 Publications Verification	Src	Cancer
DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC₅₀ of 3nM. DGY-06-116 inhibits FGFR1 with an IC₅₀ of 8340 nM .

HY-128798

Menin-MLL inhibitor 20	Epigenetic Reader Domain	Cancer
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, Intermediate 6) .

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-148159

Safrazine	Monoamine Oxidase	Neurological Disease
Safrazine is an irreversible, non-specific and orally active monoamine oxidase (MAO) inhibitor. Safrazine can be used for the research of depression .

HY-105999B

APC 366 TFA

Others Others

APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases .

APC 366 TFA	Others	Others
APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases .

HY-146341

FAAH-IN-5	FAAH MAGL	Neurological Disease
FAAH-IN-5 (Compound 7) is a relative selective, irreversible fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ of 10.5 nM. FAAH-IN-5 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability .

HY-W019847

Azamulin	Cytochrome P450	Infection Metabolic Disease
Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC₅₀ values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .

HY-B0334

Sulbactam 5+ Cited Publications CP45899	Bacterial Antibiotic	Infection
Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .

HY-B0334A

Sulbactam sodium 5+ Cited Publications CP45899 sodium	Bacterial Antibiotic	Infection
Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .

HY-112995

Lepirudin	Thrombin	Inflammation/Immunology
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT) .

HY-141677

INCB059872	Histone Demethylase	Cancer
INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia .

HY-141677A

INCB059872 dihydrochloride	Histone Demethylase	Cancer
INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .

HY-147250A

Lirafugratinib hydrochloride RLY-4008 hydrochloride	FGFR	Cancer
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-147250

Lirafugratinib RLY-4008	FGFR	Cancer
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-19985

PF-06459988	EGFR	Cancer
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .

HY-12534

Wiskostatin 1 Publications Verification	Arp2/3 Complex	Neurological Disease
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels .

HY-146342

FAAH/MAGL-IN-3	FAAH MAGL	Neurological Disease
FAAH/MAGL-IN-3 (Compound 10) is an irreversible fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) dual inhibitor with IC₅₀ values of 179 and 759 nM against FAAH and MAGL, respectively. FAAH/MAGL-IN-3 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability .

HY-152108

SARS-CoV-2 Mpro-IN-6	SARS-CoV	Infection
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M ^pro inhibitor with an IC₅₀ of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .

HY-116042

FSCPX	Adenosine Receptor	Cardiovascular Disease
FSCPX is a potent and selective irreversible antagonist of A₁ adenosine receptor (A₁AR), with low nanomolar potency for binding to the A₁AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .

HY-108908

(Rac)-Modipafant UK-74505	Flavivirus Dengue virus	Infection Inflammation/Immunology
(Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection .

HY-121450

Lavoltidine Loxtidine; AH-234844	Histamine Receptor	Cancer
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia .

HY-141680

CPS2 1 Publications Verification	PROTACs CDK	Cancer
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC₅₀= 24 nM). CPS2 can be used for the research of acute myeloid leukemia .

HY-P0034A

Ac-DEVD-CMK TFA 1 Publications Verification Caspase-3 Inhibitor III TFA	Caspase Apoptosis	Metabolic Disease
Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK TFA significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK TFA can be used in a variety of experimental approaches to inhibit apoptosis .

HY-144676

pan-HER-IN-1	EGFR Apoptosis	Cancer
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC₅₀ values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR ^T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities .

HY-18930

NU6300	CDK	Cancer
NU6300 is a covalent, irreversible and ATP-competitive CDK2 inhibitor with an IC₅₀ value of 0.16 μM. NU6300 can be used for the research of eukaryotic cell cycle- and transcription-related .

HY-143319

SPH5030	Others	Cancer
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 ^WT and EGFR ^WT with IC₅₀s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .

HY-109143

Elsubrutinib ABBV-105	Btk	Inflammation/Immunology
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC₅₀ of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .

HY-114436

MRTX-1257 3 Publications Verification	Ras	Cancer
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-W017423

(-)-Carvone	Cholinesterase (ChE)	Neurological Disease
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae .

HY-115673

LAS17 1 Publications Verification	Glutathione S-transferase	Cancer
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-139915

MPO-IN-1	Glutathione Peroxidase	Inflammation/Immunology
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC₅₀s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation .

HY-132817

Gunagratinib ICP-192	FGFR	Cancer
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer . Gunagratinib 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-142032

RBM10-8	LPL Receptor	Inflammation/Immunology
RBM10-8 is irreversible inhibitor of recombinant human sphingosine-1-phosphate lyase (hS1PL) . Sphingosine-1-phosphate (S1P) is a sphingolipid (SL) that acts as a signaling molecule regulating diverse cellular processes such as cell proliferation and differentiation, angiogenesis, immune function, inflammation, and development .

HY-155671

HDAC6-IN-18	HDAC	Cancer
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC₅₀ values of 0.17, 0.7 and 0.42 μM, respectively .

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Proteasome	Cancer
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-139504

Gamcemetinib CC-99677	MAPKAPK2 (MK2)	Inflammation/Immunology
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC₅₀=156.3 nM) and cell based assays (EC₅₀=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .

HY-155693

Topoisomerase II inhibitor 16	Topoisomerase Parasite	Infection
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research .

HY-110130

RN-1 dihydrochloride	Histone Demethylase	Cardiovascular Disease Cancer
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC₅₀ values of 0.51 μM and 2.785 μM respectively .

HY-50202A

Etomoxir sodium salt 60+ Cited Publications (R)-(+)-Etomoxir sodium salt	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-134318B

8-Azido-ADP disodium	DNA/RNA Synthesis	Others
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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus

2988 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 2988 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

1670 compounds

MCE covalent inhibitor library contains 1670 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.

Cat. No.	Product Name	Target	Research Area

HY-P0034A

Ac-DEVD-CMK TFA 1 Publications Verification Caspase-3 Inhibitor III TFA	Caspase Apoptosis	Metabolic Disease
Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK TFA significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK TFA can be used in a variety of experimental approaches to inhibit apoptosis .

HY-137495

GGACK

PAI-1 Ser/Thr Protease Cancer

GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .

HY-112995

Lepirudin	Thrombin	Inflammation/Immunology
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT) .

HY-W796158

Z-DEVD-CMK

Cathepsin Inflammation/Immunology

Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro .

HY-P3648

Ala-Ala-Pro-Val-chloromethylketone AAPV-CMK	Elastase	Inflammation/Immunology
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases .

HY-P5989

Calpain inhibitor V Mu-Val-HPh-FMK	Antibiotic	Infection
Calpain inhibitor V (Mu-Val-HPh-FMK) is a cell-permeable and irreversible inhibitor of calpain that has anti-chlamydial activity .

HY-P1182

C21

Histone Methyltransferase Cancer

C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC₅₀ of 1.8 μM. C21 inhibits PRMT6 with an IC₅₀ of 8.8 μM .

HY-134161

DL-α-(Difluoromethyl)arginine	Peptides	Metabolic Disease
DL-α-(Difluoromethyl)arginine is an potent, enzyme-activated and irreversible arginine decarboxylases inhibitor. DL-α-(Difluoromethyl)arginine blocks the arginine decarboxylase activity of E.coli and Pseudomonas aeruginosa in vivo .

HY-P5855

μ-Conotoxin SxIIIC	Sodium Channel	Neurological Disease
μ-Conotoxin SxIIIC is an irreversible Na_V channel inhibitor that can be obtained from the Conus striolatus. μ-Conotoxin SxIIIC can be used in the study of neurological diseases such as chronic pain .

HY-137330

S-(2,4-Dinitrophenyl)glutathione	Endogenous Metabolite	Metabolic Disease
S-(2,4-Dinitrophenyl)glutathione is a substrate for glutathione-S-transferase. (2,4-Dinitrophenyl)glutathione can be used as an irreversible glutathione reductase inhibitor with an K_i value of 30 µM .

HY-105019

Melflufen Melphalan flufenamide	DNA Alkylator/Crosslinker Apoptosis	Cancer
Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells .

HY-P2233

Globomycin	Bacterial Antibiotic	Infection
Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute *Spiroplasma melliferum* with a MIC in the range 6.25-12.5 μM .

HY-P1010

Z-LEHD-FMK Maximum Cited Publications 7 Publications Verification	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-P5062

DEC-RVRK-CMK Decanoyl-Arg-Val-Arg-Lys-chloromethylketone	Peptides	Infection
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a small, synthetic, irreversible, cell-permeable competitive furin inhibitor against Zika virus (ZIKV), Japanese encephalitis virus (JEV) has strong antiviral activity .

HY-P1407

Z-VRPR-FMK TFA VRPR	MALT1 Influenza Virus	Infection Cancer
Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection .

HY-P1010A

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

HY-P1007

Z-VEID-FMK Z-VE(OMe)ID(OMe)-FMK	Caspase Apoptosis	Cancer
Z-VEID-FMK (Z-VE(OMe)ID(OMe)-FMK) is a selective and irreversible caspase-6 peptide inhibitor. Z-VEID-FMK alleviates the S-(+)-ketamine-induced augmentation of caspase-6 activity, DNA fragmentation, and cell apoptosis .

HY-P2837

Oxaloacetate decarboxylase	Endogenous Metabolite	Metabolic Disease
Oxaloacetate decarboxylase catalyzes the irreversible decarboxylation of oxaloacetate to pyruvate and COIC₂. Oxaloacetate decarboxylase is a member of the sodium ion transport decarboxylase (NaT-DC) enzyme family. Oxaloacetate decarboxylase converts the chemical energy of the decarboxylation reaction into an electrochemical gradient of Na ⁺ ions across the membrane .

HY-P4900

Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone	Caspase	Others
Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone is a cell-permeable, non-toxic inhibitor that binds irreversibly to activated caspase-3 in apoptotic cells. The fluorescence intensity can be measured by flow cytometry, microwell plate reader, or fluorescence microscopy .

HY-P0111

Z-WEHD-FMK 2 Publications Verification Z-WE(OMe)HD(OMe)-FMK	Caspase Cathepsin	Cancer
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC₅₀=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W017423

(-)-Carvone	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source classification Gymnaster koraiensis Plants Umbelliferae	Cholinesterase (ChE)
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae .

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Marine natural products Source classification Marine microorganism	Proteasome
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-B0221

Amphotericin B 10+ Cited Publications	Infection Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Disease Research Fields	Fungal Antibiotic Bacterial Parasite
Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.

HY-B1122

L-Cycloserine (S)-Cycloserine; (S)-4-Amino-3-isoxazolidone	Structural Classification Microorganisms Neurological Disease Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics Cancer	GABA Receptor HIV
L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminitransferase in E.

HY-N1638

1-Methyl-2-undecyl-4(1H)-quinolone	Alkaloids Source classification Evodia rutaecarpa (Juss.) Benth. Rutaceae Quinoline Alkaloids Plants	Monoamine Oxidase
1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC₅₀ and K_i values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .

HY-N6781

Ophiobolin A	Infection Microorganisms Classification of Application Fields Terpenoids Sesquiterpenes Source classification Disease Research Fields	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-N1283

Seneciphyllinine	Alkaloids other families Pyrrole Alkaloids Classification of Application Fields Source classification Metabolic Disease Plants Disease Research Fields	Others
Seneciphyllinine, a pyrrolizidine alkaloid, is isolated from the roots of Gynura japonica. Pyrrolizidine alkaloids are highly hepatotoxic natural chemicals that produce irreversible chronic and acute hepatotoxic effects on human beings .

HY-Y1750A

β-Aminopropionitrile hydrochloride BAPN hydrochloride	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Cancer	Monoamine Oxidase Endogenous Metabolite
β-Aminopropionitrile (BAPN) hydrochloride is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile hydrochloride targets the active site of LOX or LOXL isoenzymes .

HY-N10686

Tanshinone IIA anhydride	Structural Classification Flavonoids Labiatae Source classification Samanea saman (Jacq.) Merr. Plants Other Flavonoids	Cholinesterase (ChE)
Tanshinone IIA anhydride is a potent and irreversible human carboxylesterase (CE) inhibitor with K_i values of 1.9 nM and 1.4 nM for human CE1 and the human intestinal CE (hiCE), respectively .

HY-N0688

Linderane	Classification of Application Fields Terpenoids Sesquiterpenes Source classification Plants Lauraceae Inflammation/Immunology Disease Research Fields Lindera aggregata (Sims) Kosterm.	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-137330

S-(2,4-Dinitrophenyl)glutathione	Structural Classification Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
S-(2,4-Dinitrophenyl)glutathione is a substrate for glutathione-S-transferase. (2,4-Dinitrophenyl)glutathione can be used as an irreversible glutathione reductase inhibitor with an K_i value of 30 µM .

HY-12686

5Z-7-Oxozeaenol 5+ Cited Publications FR148083; L783279; LL-Z 1640-2	Structural Classification Natural Products Monophenols Microorganisms Classification of Application Fields Source classification Phenols Inflammation/Immunology Disease Research Fields	MAP3K VEGFR Antibiotic
5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC₅₀s of 8 nM and 52 nM, respectively.

HY-B0221R

Amphotericin B (Standard)	Infection Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Disease Research Fields	Fungal Antibiotic Bacterial Parasite
Amphotericin B (Standard) is the analytical standard of Amphotericin B. This product is intended for research and analytical applications. Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.

HY-W012875

3-Nitropropanoic acid β-Nitropropionic acid; Bovinocidin	Structural Classification Microorganisms other families Classification of Application Fields Ketones, Aldehydes, Acids Source classification Metabolic Disease Plants Disease Research Fields	Bacterial Apoptosis Autophagy
3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible and orally active inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM. 3-Nitropropanoic acid can induce cell apoptosis .

HY-N5142

α-Terpineol	Structural Classification Classification of Application Fields Source classification Plants Infection Other Monoterpenes Saururaceae Microorganisms Terpenoids Myrtaceae Eucalyptus globulus Labill. Inflammation/Immunology Disease Research Fields	Bacterial
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria . α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption .

HY-131394

5-Hydroxymethyl-2’-deoxycytidine 5hmdC	Structural Classification Natural Products Classification of Application Fields Animals Source classification Disease Research Fields Cancer	Others
5-Hydroxymethyl-2’-deoxycytidine (5hmdC) is an oxidation derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA. 5-Hydroxymethyl-2’-deoxycytidine may serve as a marker of irreversibly damaged cells .

HY-130430

Neplanocin A (-)-Neplanocin A	Structural Classification Natural Products 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-B0470

Neomycin sulfate Maximum Cited Publications 23 Publications Verification	Structural Classification Classification of Application Fields Source classification Antibacterial Disease Research Other Antibiotics Infection Microorganisms Antibiotics Animal Husbandry Mammalian Cell Culture Anticancer Disease Research Fields	Bacterial Antibiotic Phospholipase
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .

HY-W016420

Fosfomycin sodium 4 Publications Verification MK-0955 sodium	Infection Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields	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-129476

L-Canaline	Infection Structural Classification other families Classification of Application Fields Source classification Amino acids Plants Endogenous metabolite Disease Research Fields	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-12546

Brevetoxin B Brevetoxin-2; PbTx-2	Natural Products Microorganisms Animals Source classification	Sodium Channel
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC₅₀=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively.

HY-13821

Epoxomicin 5+ Cited Publications BU-4061T	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-134664

8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate	Structural Classification Terpenoids Sesquiterpenes Source classification Plants Compositae Vachellia nilotica (L.) P. J. H. Hurter & Mabb.	Cytochrome P450 Monoamine Oxidase
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC₅₀s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC₅₀s of 60.2 and 38.6 μM, respectively .

HY-16594

Lactacystin 2 Publications Verification	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Proteasome Apoptosis ROS Kinase
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC₅₀ = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on ^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7] ^[8] ^[9] ^[10].

HY-N0110

Palmatine chloride 5 Publications Verification	Alkaloids Structural Classification Phellodendron amurense Rupr. Classification of Application Fields Source classification Rutaceae Plants Isoquinoline Alkaloids Disease Research Fields Cancer	Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-N0110B

Palmatine hydroxide 5 Publications Verification	Alkaloids Phellodendron amurense Rupr. Source classification Rutaceae Plants	Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-N0110R

Palmatine chloride (Standard)	Structural Classification Alkaloids Phellodendron amurense Rupr. Classification of Application Fields Source classification Rutaceae Plants Disease Research Fields Cancer	Apoptosis Virus Protease Indoleamine 2,3-Dioxygenase (IDO) Parasite Bacterial Aurora Kinase
Palmatine (chloride) (Standard) is the analytical standard of Palmatine (chloride). This product is intended for research and analytical applications. Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

Cat. No.	Product Name	Chemical Structure

HY-17600S

Acalabrutinib-d4
Acalabrutinib-d₄ is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 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-10997S

Ibrutinib-d5

Ibrutinib-d₅ is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor[1].
HY-14654S

Aspirin-d3

Aspirin-d₃ is the deuterium labeled Aspirin. Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.

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-10455S

Carfilzomib-d8

Carfilzomib-d₈ is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
HY-14654S1

Aspirin-d4

Aspirin-d₄ is the deuterium labeled Aspirin. Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL[1][2].

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-B0431AS

Phenoxybenzamine-d5 hydrochloride
Phenoxybenzamine-d₅ (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].

HY-B0334AS

Sulbactam-d5 sodium
Sulbactam-d₅ (sodium) is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].

HY-32721S

Neratinib-d6
Neratinib-d₆ (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

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[1].

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[1].

HY-B0431S

Phenoxybenzamine-d5
Phenoxybenzamine-d₅ is the deuterium labeled Phenoxybenzamine[1]. Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[2][3].

HY-B0221S

Amphotericin B-13C6
Amphotericin B- ¹³C₆ is ¹³C labeled Amphotericin B (HY-B0221). Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.

HY-B0334AS1

Sulbactam-d2 sodium
Sulbactam-d₂ (sodium) is the deuterium labeled Sulbactam sodium[1]. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[2][3].

HY-13632S

Exemestane-d2
Exemestane-d₂ is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].

HY-17447SA

Tranylcypromine-d5 hydrochloride

Tranylcypromine-d₅ (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].

HY-13632S2

Exemestane-d3
Exemestane-d₃ is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].

HY-B0431AS1

Phenoxybenzamine (benzyl-2,3,4,5,6-d5) (hydrochloride)
Phenoxybenzamine (benzyl-2,3,4,5,6-d₅) (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].

HY-70013S

Abiraterone-d4
Abiraterone-d₄ is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.

HY-13632S1

Exemestane-13C3
Exemestane- ¹³C₃ is the ¹³C-labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].

HY-10261S1

Afatinib-d4
Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

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-10261AS

Afatinib-d6 dimaleate
Afatinib-d₆ (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].

HY-A0061S

Trifluridine-13C,15N2
Trifluridine- ¹³C, ¹⁵N₂ is the ¹³C and ¹⁵N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].

HY-B0656S

Rabeprazole-d4
Rabeprazole-d₄ is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].

HY-B0033S

Vigabatrin-13C,d2 hydrochloride

Vigabatrin- ¹³C,d₂ (hydrochloride) is the ¹³C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].

HY-B0656AS

Rabeprazole-d4 sodium

Rabeprazole-d₄ (sodium) is the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].

HY-N5142S

α-Terpineol-d3
α-Terpineol-d₃ is the deuterium labeled α-Terpineol[1]. α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria[2].α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption[2].

HY-14605BS

Rasagiline-13C3 mesylate racemic

Rasagiline- ¹³C₃ (mesylate racemic) is a ¹³C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) 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-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-B0656AS1

Rabeprazole-d3 sodium

Rabeprazole-d₃ (sodium)mis the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].

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-14605S

Rasagiline-13C3 mesylate
Rasagiline- ¹³C₃ ((R)-AGN1135- ¹³C₃; TVP1012- ¹³C₃) mesylateis the deuterium labeledRasagiline (mesylate)(HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively .

HY-B1075AS

(Rac)-Fosfomycin (benzylamine)-13C3

(Rac)-Fosfomycin (benzylamine)- ¹³C₃ is the ¹³C labeled Fosfomycin[1]. 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[2][3].

HY-135334S

ACP-5862-d4
ACP-5862-d₄ is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].

HY-17447AS

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

(1S,2R)-Tranylcypromine-d₅ (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride[1]. 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[2][3][4].

Cat. No.	Product Name		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-A0091

Pargyline hydrochloride 2 Publications Verification		Alkynes
Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with K_is of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline hydrochloride has antihypertensive and anticancer activities . Pargyline (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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

HY-151645

Alkyne-SNAP		Alkynes Labeling and Fluorescence Imaging
Alkyne-SNAP (compound 3) is an Alkyne-conjugated benzylguanine. The benzylguanine moiety reacts with the SNAP-tag, allowing irreversible and covalent labeling of SNAP fusion proteins with an additional alkyne functionality for further click chemistry conjugation .

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-A0091A

Pargyline 2 Publications Verification		Alkynes
Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with K_is of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities . Pargyline 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-120330

Nek2-IN-5		Alkynes
Nek2-IN-5 (compound 6) is a potent and irreversible Nek2 ((Never in mitosis gene a)-related kinase 2) inhibitior . Nek2-IN-5 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-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-14605

Rasagiline mesylate 5 Publications Verification (R)-AGN1135 mesylate; TVP1012 mesylate		Alkynes
Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-14605A

Rasagiline 5 Publications Verification (R)-AGN1135; TVP1012		Alkynes
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-14605BS

Rasagiline-13C3 mesylate racemic AGN1135-¹³C₃; TVP1012-¹³C₃ racemic		Alkynes
Rasagiline- ¹³C₃ (mesylate racemic) is a ¹³C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) 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-10533

Eniluracil 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-116423

JH295		Alkynes
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 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-116423A

JH295 hydrate		Alkynes
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) 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-151646

Alkyne-PEG5-SNAP		Alkynes Labeling and Fluorescence Imaging
Alkyne-PEG5-SNAP is a click chemistry reagent containing an alkyne group. Alkyne-PEG5-SNAP can alkyne conjugated benzylguanine (BG), the BG moiety reacts specifically and rapidly with SNAP-tag, a polypeptide protein tag, allowing irreversible and covalent labeling of SNAP fusion proteins with an additional alkyne functionality suitable for further conjugation . Alkyne-PEG5-SNAP 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-126781

Fozivudine tidoxil BM-211290		Azide
Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of agent, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription . Fozivudine tidoxil 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

HY-146314

MAO-B-IN-9		Alkynes
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC₅₀ of 0.18 μM. MAO-B-IN-9 prevents Aβ_1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ_1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-131036

MAO-IN-M30 dihydrochloride		Alkynes
MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC₅₀=37 nM) and MAO-B (IC₅₀=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease . MAO-IN-M30 (dihydrochloride) 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-146677

5-HT6R/MAO-B modulator 1		Alkynes
5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT₆R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits . 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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