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Results for "

Irreversible Inhibitors

" in MCE Product Catalog:

363

Inhibitors & Agonists

2

Screening Libraries

1

Biochemical Assay Reagents

11

Peptides

16

Natural
Products

30

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-151878
    CDK7-IN-20

    		CDK GSK-3 Metabolic Disease
    CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.
  • HY-147691
    MPO-IN-5

    		Glutathione Peroxidase Potassium Channel Inflammation/Immunology
    MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1.
  • HY-112823A
    Almonertinib mesylate

    HS-10296 mesylate

    		 EGFR Cancer
    Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
  • HY-103334
    MAFP

    Methyl Arachidonyl Fluorophosphonate

    		 Phospholipase Metabolic Disease Neurological Disease Cardiovascular 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-101868
    INF39

    		NOD-like Receptor (NLR) Inflammation/Immunology
    INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.
  • HY-122543A
    PPACK II

    		Ser/Thr Protease Cardiovascular Disease
    PPACK II is an irreversible and specific glandular and plasma kallikreins inhibitor.
  • HY-122543
    PPACK II diTFA

    		Ser/Thr Protease Cardiovascular Disease
    PPACK II diTFA is an irreversible and specific glandular and plasma kallikreins inhibitor.
  • HY-12821
    AEBSF hydrochloride

    		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-112274
    M443

    		Others Cancer
    M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.
  • HY-100944
    Conduritol B epoxide

    		Glucosidase Neurological Disease
    Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.
  • HY-100520
    EGFR-IN-2

    		EGFR Cancer
    EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
  • HY-112570
    CC-90003

    		ERK Cancer
    CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
  • HY-B0496
    PMSF

    Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride

    		 Cathepsin Others
    PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
  • HY-103389
    1-Aminobenzotriazole

    ABT; 3-Aminobenzotriazole

    		 Cytochrome P450 Cancer
    1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).
  • HY-17632
    Tarloxotinib bromide

    TH-4000

    		 EGFR Cancer
    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  • HY-10997S
    Ibrutinib-d5

    PCI-32765-d5

    		 Btk Cancer
    Ibrutinib-d5 is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor[1].
  • HY-A0006
    Pentostatin

    CI-825; Deoxycoformycin

    		 Adenosine Deaminase Antibiotic Cancer
    Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with Ki of 2.5 pM.
  • HY-100335
    PCI-33380

    		Btk Others
    PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
  • HY-B1199
    Nialamide

    		Monoamine Oxidase Neurological Disease
    Nialamide is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class that was used as an antidepressant.
  • HY-10261S
    Afatinib D6

    BIBW 2992 d6

    		 EGFR Autophagy Cancer
    Afatinib-d6 is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor[1].
  • HY-133110
    Afatinib N-Oxide

    		Drug Metabolite Others
    Afatinib N-Oxide is an impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
  • HY-14197A
    Clorgyline hydrochloride

    		Monoamine Oxidase Metabolic Disease
    Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) that is used in scientific research; structurally related to Pargyline.
  • HY-52101A
    FMK

    		Ribosomal S6 Kinase (RSK) Cancer
    FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
  • HY-B0531
    Triflusal

    		COX Inflammation/Immunology
    Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.
  • 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-115733
    Cathepsin L-IN-2

    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-15282
    E-64

    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-10997A
    Ibrutinib Racemate

    PCI-32765 Racemate

    		 Btk Cancer
    Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
  • HY-19816A
    Avitinib maleate

    Abivertinib maleate; AC0010 maleate

    		 EGFR Cancer
    Avitinib (Abivertinib) maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM.
  • HY-12466
    Z-DEVD-FMK

    		Caspase Cancer
    Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with an IC50 of 18 μM.
  • HY-12015
    Iniparib

    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-B1235
    Acetohydroxamic acid

    N-Hydroxyacetamide

    		 Bacterial Infection
    Acetohydroxamic acid is a potent and irreversible inhibitor of bacterial and plant urease and also used as adjunctive therapy in chronic urinary infection.
  • HY-10997
    Ibrutinib

    PCI-32765

    		 Btk Ligands for Target Protein for PROTAC Cancer
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-16658
    Z-VAD(OMe)-FMK

    Z-Val-Ala-Asp(OMe)-FMK

    		 Caspase Cancer
    Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a cell-permeable and irreversible pan-caspase inhibitor. Z-VAD(OMe)-FMK is an ubiquitin carboxy-terminal hydrolase L1 (UCHL1) inhibitor. Z-VAD(OMe)-FMK irreversibly modifies UCHL1 by targeting the active site of UCHL1.
  • HY-111341
    AZD5904

    		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-103085
    T-3775440 hydrochloride

    		Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
  • HY-101267
    CHMFL-BMX-078

    CHMFL-BMX 078

    		 BMX Kinase Cancer
    CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.
  • HY-13897
    CNX-2006

    		EGFR Cancer
    CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFR T790M.
  • 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-10455
    Carfilzomib

    PR-171

    		 Proteasome Autophagy Apoptosis Cancer
    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-B0886A
    Iproniazid

    		Monoamine Oxidase Neurological Disease
    Iproniazid is a non-selective, irreversible monoamine oxidase (MAO) inhibitor of the hydrazine class. Iproniazid has antidepressive activity.
  • HY-100546A
    GSK-LSD1 dihydrochloride

    		Histone Demethylase Monoamine Oxidase Cancer
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
  • HY-10325
    CL-387785

    EKI-785; WAY-EKI 785

    		 EGFR Cancer
    CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.
  • HY-121493
    TM2-115

    		Histone Methyltransferase Parasite Infection
    TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.
  • HY-152232
    BChE-IN-15

    		Cholinesterase (ChE) Cancer
    BChE-IN-15 (Compound 6) is a pseudo-irreversible and covalent BChE inhibitor with an IC50 of 1.76 nM against hBChE .
  • HY-100894
    Biotin-VAD-FMK

    		Caspase Cancer
    Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
  • HY-B0886
    Iproniazid phosphate

    		Monoamine Oxidase Neurological Disease
    Iproniazid phosphate is a non-selective, irreversible monoamine oxidase (MAO) inhibitor of the hydrazine class. Iproniazid phosphate has antidepressive activity.
  • HY-131705
    BTK inhibitor 17

    		Btk Inflammation/Immunology
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
  • HY-126765
    Territrem B

    		Cholinesterase (ChE) Infection Neurological Disease
    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-B0744
    Eflornithine

    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-U00197
    Tilmacoxib

    JTE522; JTP19605; RWJ57504

    		 COX Inflammation/Immunology
    Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
  • HY-B0744A
    Eflornithine hydrochloride

    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-18605
    K-Ras G12C-IN-2

    		Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  • 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-146657
    4BAB

    		Glyoxalase (GLO) Cancer
    4BAB (compound 29) is an irreversible glyoxalase I (GLO1) inhibitor. 4BAB has anticancer effects.
  • HY-107841
    K-Ras(G12C) inhibitor 6

    		Ras Cancer
    K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C).
  • HY-13229
    BOC-D-FMK

    		Caspase Apoptosis Cancer
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
  • 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-13929
    Isocarboxazid

    		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-148375
    Abiraterone sulfate

    		Drug Metabolite Others
    Abiraterone sulfate is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity.
  • HY-17646
    Verdiperstat

    AZD3241

    		 Glutathione Peroxidase Neurological Disease
    Verdiperstat (AZD3241) is a selective, irreversible and orally active myeloperoxidase (MPO) inhibitor, with an IC50 of 630 nM, and can be used in the research of neurodegenerative brain disorders.
  • HY-18606
    K-Ras G12C-IN-3

    		Ras Cancer
    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
  • 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.
  • HY-101976
    JAK3-IN-6

    		JAK Inflammation/Immunology
    JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
  • HY-17600S
    Acalabrutinib-d4

    ACP-196-d4

    		 Btk Cancer
    Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1].
  • HY-136605
    DGY-06-116

    		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-102087
    JPM-OEt

    		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-12782T
    Iadademstat dihydrochloride

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

    		 Histone Demethylase Cancer
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • 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-78727
    Ibrutinib deacryloylpiperidine

    IBT4A

    		 Btk Cancer
    Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-148376
    Abiraterone N-oxide

    		Drug Metabolite Cancer
    Abiraterone N-oxide is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity.
  • HY-B0880
    4-Aminobenzohydrazide

    p-Aminobenzohydrazide; p-Aminobenzoic acid hydrazide

    		 Glutathione Peroxidase Neurological Disease
    4-Aminobenzohydrazide is an irreversible MPO myeloperoxidase inhibitor with an IC50 of 0.3 µM. It is used for the research of subacute stroke.
  • HY-75054
    Abiraterone acetate

    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-14605BS
    Rasagiline-13C3 mesylate racemic

    AGN1135-13C3; TVP1012-13C3 racemic

    		 Monoamine Oxidase Neurological Disease
    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].
  • 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-10397A
    MX1013

    CV1013; Z-VD-FMK

    		 Caspase Cancer
    MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM.
  • HY-B0744B
    Eflornithine hydrochloride hydrate

    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-19803
    Naquotinib mesylate

    ASP8273 (mesylate)

    		 EGFR Cancer
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-133740
    MS117

    		Histone Methyltransferase Cancer
    MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.
  • 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-B1122
    L-Cycloserine

    (S)-Cycloserine; (S)-4-Amino-3-isoxazolidone

    		 GABA Receptor HIV Neurological Disease Cancer
    L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminitransferase in E.
  • HY-19729
    Naquotinib

    ASP8273

    		 EGFR Cancer
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-19816
    Avitinib

    Abivertinib; AC0010

    		 EGFR Btk Cancer
    Avitinib (AC0010) is an irreversible, mutant-selective EGFR inhibitor that effectively inhibits EGFR T790M resistance mutations in non-small cell lung cancer (NSCLC). Abivertinib is also a novel BTK inhibitor.
  • HY-32721
    Neratinib

    HKI-272

    		 EGFR Cancer
    Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
  • HY-18632
    GSK2879552

    		Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
  • HY-32721B
    Neratinib maleate

    HKI-272 maleate

    		 EGFR Cancer
    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
  • HY-136113
    Ibrutinib dimer

    		Btk Cancer
    Ibrutinib dimer is a Dimer of Ibrutinib. Ibrutinib dimer is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-12305A
    (R)-Q-VD-OPh

    (R)-QVD-OPH; (R)-Quinoline-Val-Asp-Difluorophenoxymethylketone

    		 Apoptosis Cancer
    (R)-Q-VD-OPh ((R)-QVD-OPH) is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible pan-caspase inhibitor with potent antiapoptotic properties.
  • HY-N6781
    Ophiobolin A

    		Phosphodiesterase (PDE) Cancer Infection
    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-10455S
    Carfilzomib-d8

    		Proteasome Autophagy Apoptosis Cancer
    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-B1368
    Fenclonine

    4-Chloro-DL-phenylalanine; PCPA; CP-10188

    		 Tryptophan Hydroxylase Cancer Neurological Disease
    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-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-110063
    4-IPP

    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-112161
    Branebrutinib

    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.
  • HY-100229
    Aloxistatin

    E64d; E64c ethyl ester

    		 Cathepsin SARS-CoV Neurological Disease
    Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
  • HY-116856
    SRPKIN-1

    		SRPK Cancer Cardiovascular Disease
    SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.
  • HY-43521
    Ibrutinib-MPEA

    		Btk Cancer
    Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies.
  • HY-14645
    (-)-DHMEQ

    Dehydroxymethylepoxyquinomicin

    		 NF-κB Cancer Inflammation/Immunology
    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.
  • HY-12029
    WZ8040

    		EGFR Cancer
    WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.
  • HY-115673
    LAS17

    		Gutathione 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.
  • HY-10396
    Emricasan

    PF 03491390; IDN-6556

    		 Caspase Influenza Virus Cancer Infection Neurological Disease
    Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors.
  • HY-50202
    Etomoxir

    (R)-(+)-Etomoxir

    		 Apoptosis Cancer Metabolic Disease
    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-119293
    K777

    		Cathepsin CCR Cytochrome P450 Cancer Infection
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
  • HY-112318
    GSK-2793660 free base

    		Cathepsin Inflammation/Immunology
    GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis.
  • HY-128352
    SMYD3-IN-1

    		Histone Methyltransferase Cancer
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  • HY-18603
    FIIN-3

    		EGFR FGFR Cancer
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
  • 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-128971
    LHVS

    		Cathepsin Parasite Infection Neurological Disease
    LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM.
  • HY-150105
    Menin-MLL inhibitor 21

    		Epigenetic Reader Domain Cancer Inflammation/Immunology
    Menin-MLL inhibitor 21(example 9) is a specific irreversible inhibitor of Menin-MLL interactions and can be used in the study of autoimmune diseases, alloimmune diseases, cancer and other diseases dependent on menin-MLL.
  • HY-100227
    E 64c

    		Cathepsin SARS-CoV Metabolic Disease
    E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
  • HY-N10686
    Tanshinone IIA anhydride

    		Cholinesterase (ChE) Cancer
    Tanshinone IIA anhydride is a potent and irreversible human carboxylesterase (CE) inhibitor with Ki values of 1.9 nM and 1.4 nM for human CE1 and the human intestinal CE (hiCE), respectively.
  • HY-14654S
    Aspirin-d3

    Acetylsalicylic Acid-d3; ASA-d3

    		 COX Autophagy Mitophagy Virus Protease Inflammation/Immunology Cancer
    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-13943
    CNX-774

    		Btk Cancer
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.
  • HY-Y1750A
    β-Aminopropionitrile hydrochloride

    BAPN hydrochloride

    		 Monoamine Oxidase Endogenous Metabolite Cancer Metabolic Disease
    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-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-Y1750
    β-Aminopropionitrile

    BAPN

    		 Monoamine Oxidase Endogenous Metabolite Cancer Metabolic Disease
    β-Aminopropionitrile (BAPN) is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes.
  • HY-32718
    Pelitinib

    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-B0218
    Orlistat

    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-120231
    Z-VRPR-FMK

    		MALT1 Cancer
    Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression.
  • HY-50202A
    Etomoxir sodium salt

    (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-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.
  • HY-114436
    MRTX-1257

    		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-18632A
    GSK2879552 dihydrochloride

    		Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • HY-A0091
    Pargyline hydrochloride

    		Monoamine Oxidase Cancer Cardiovascular Disease
    Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline hydrochloride has antihypertensive and anticancer activities.
  • HY-B0744C
    L-Eflornithine

    L-DFMO; L-RMI71782; L-α-difluoromethylornithine

    		 Parasite Cancer
    L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-18604
    K-Ras G12C-IN-1

    		Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
  • HY-114304
    COH000

    		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-A0091A
    Pargyline

    		Monoamine Oxidase Cancer Cardiovascular Disease
    Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities.
  • HY-125006
    TRi-1

    		Others 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-W012875
    3-Nitropropanoic acid

    β-Nitropropionic acid; Bovinocidin

    		 Bacterial Apoptosis Infection Metabolic Disease
    3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM.
  • HY-12823
    BLU9931

    		FGFR Cancer
    BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity.
  • HY-12534
    Wiskostatin

    		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-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-B0334
    Sulbactam

    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-19730
    Olmutinib

    HM61713, BI 1482694

    		 EGFR Cancer
    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.
  • HY-13272
    Dacomitinib

    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-128903
    MC-Val-Cit-PAB-carfilzomib iodide

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-carfilzomib iodide is a agent-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • 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-151200
    Steroid sulfatase-IN-4

    		Others Endocrinology
    Steroid sulfatase-IN-4 (Compound 16) is an irreversible steroid sulfatase (STS) inhibitor with an IC50 of 25 nM against human STS. Steroid sulfatase-IN-4 can be used for the research of endometriosis.
  • HY-128867
    bio-THZ1

    		CDK Cancer
    bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
  • HY-B0334A
    Sulbactam sodium

    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-124628
    IPI-9119

    		Fatty Acid Synthase (FASN) Cancer
    IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.
  • HY-13734
    PX-12

    IV-2

    		 Others 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-117068
    (R)-Bromoenol lactone

    (R,E)-Bromoenol lactone

    		 Phospholipase Others
    (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 µM.
  • HY-148281
    TMX-2164

    		Bcl-2 Family Cancer
    TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells.
  • HY-B0744D
    L-Eflornithine monohydrochloride

    L-DFMO monohydrochloride; ; L-RMI71782 monohydrochloride; L-α-difluoromethylornithine monohydrochloride

    		 Parasite Cancer
    L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
  • HY-13731
    PPI-2458

    		Others Cancer Inflammation/Immunology
    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-75054S
    Abiraterone acetate-d4

    CB7630-d4

    		 Isotope-Labeled Compounds Cytochrome P450 Cancer
    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-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 Ki value of 30 µM.
  • HY-138794
    XL177A

    		Deubiquitinase Cancer
    XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism.
  • HY-14654S1
    Aspirin-d4

    Acetylsalicylic Acid-d4; ASA-d4

    		 COX Autophagy Mitophagy Virus Protease Inflammation/Immunology Cancer
    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-112665
    Virginiamycin Complex

    Streptogramin; Mikamycin; RP 7293

    		 Antibiotic Bacterial Infection
    Virginiamycin complex contains two streptogramin antibiotics, virginiamycin M1 and virginiamycin S1 produced by S. virginiae. As a complex, the two antibiotics act synergistically to irreversibly inhibit protein synthesis in bacteria.
  • HY-10367A
    Canertinib dihydrochloride

    CI-1033 dihydrochloride; PD-183805 dihydrochloride

    		 EGFR Orthopoxvirus Cancer Infection
    Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice.
  • HY-129126
    NC9

    Cbz-Lys(Acr)-PEG2-dansyl

    		 Glutaminase Microtubule/Tubulin Others
    NC9 (Cbz-Lys(Acr)-PEG2-dansyl) is an irreversible transglutaminase (TG) inhibitor. NC9 inhibits osteoblast differentiation and mineralization. NC9 destabilizes microtubules. NC9 can be used for the research of osteoblast differentiation.
  • HY-103443
    HKI-357

    		EGFR Cancer
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
  • 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-14605
    Rasagiline mesylate

    (R)-AGN1135 mesylate; TVP1012 mesylate

    		 Monoamine Oxidase Autophagy Apoptosis Neurological Disease
    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-14605A
    Rasagiline

    (R)-AGN1135; TVP1012

    		 Monoamine Oxidase Neurological Disease
    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.
  • HY-101521
    CHMFL-BTK-01

    		Btk Cancer
    CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC50 of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation.
  • HY-101564
    Onametostat

    JNJ-64619178

    		 Histone Methyltransferase Cancer
    Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer.
  • HY-112205A
    RR-11a analog

    		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-B0033
    Vigabatrin hydrochloride

    γ-Vinyl-GABA hydrochloride

    		 GABA Receptor Neurological Disease
    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.
  • HY-70013
    Abiraterone

    CB-7598

    		 Cytochrome P450 Cancer
    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-15399
    Vigabatrin

    γ-Vinyl-GABA

    		 GABA Receptor Neurological Disease
    Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
  • HY-144464
    SARS-CoV-2 Mpro-IN-1

    		SARS-CoV Infection
    SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective and irreversible inhibitor of SARS-CoV-2 main protease (Mpro), with an IC50 of 116 nM.
  • HY-13036A
    IBT6A

    		Btk Cancer
    IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-131693
    γ-Acetylenic GABA

    4-Aminohex-5-ynoic acid

    		 GABA Receptor Neurological Disease
    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.
  • HY-105019A
    Melflufen hydrochloride

    Melphalan flufenamide hydrochloride

    		 DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-13036B
    IBT6A hydrochloride

    		Btk Cancer
    IBT6A hydrochloride is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • 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-137193
    5,6-Dihydroabiraterone

    		Drug Metabolite Cancer
    5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer).
  • HY-112847A
    Sulfosuccinimidyl oleate sodium

    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-112847
    Sulfosuccinimidyl oleate

    Sulfo-N-succinimidyl oleate

    		 Mitophagy Inflammation/Immunology
    Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
  • HY-151523
    KRas G12R inhibitor 1

    		Ras Cancer
    KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research.
  • HY-136526
    BCR-ABL-IN-3

    		Bcr-Abl Cancer
    BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity.
  • HY-14200
    (S)-Rasagiline

    TVP1022; S-PAI

    		 Monoamine Oxidase Neurological Disease
    (S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, 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-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-A0061
    Trifluridine

    Trifluorothymidine; 5-Trifluorothymidine; TFT

    		 Thymidylate Synthase HSV Nucleoside Antimetabolite/Analog Orthopoxvirus Cancer
    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.
  • HY-14200A
    (S)-Rasagiline mesylate

    TVP1022 mesylate; S-PAI mesylate

    		 Monoamine Oxidase Neurological Disease
    (S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
  • HY-109061
    Lazertinib

    YH25448; GNS-1480

    		 EGFR Cancer
    Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung 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-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-135815
    Mobocertinib

    TAK-788; AP32788

    		 EGFR Cancer
    Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research.
  • HY-135815B
    Mobocertinib mesylate

    TAK-788 mesylate; AP32788 mesylate

    		 EGFR Cancer
    Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
  • 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-141480
    GSK-3β inhibitor 3

    		GSK-3 Apoptosis Cancer
    GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
  • HY-P1010
    Z-LEHD-FMK

    		Caspase Apoptosis Cancer Neurological Disease
    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-12686
    5Z-7-Oxozeaenol

    FR148083; L783279; LL-Z 1640-2

    		 MAP3K VEGFR Antibiotic Infection Inflammation/Immunology
    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-10367
    Canertinib

    CI-1033; PD-183805

    		 EGFR Orthopoxvirus Cancer Infection
    Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.
  • 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-120986
    (S)-Bromoenol lactone

    (S)-BEL; (S,E)-Bromoenol lactone

    		 Phospholipase Inflammation/Immunology
    (S)-Bromoenol lactone ((S)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase A2β (iPLA2β) that inhibits the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells with an IC50 of 2 µM.
  • HY-133118
    6RK73

    		Deubiquitinase Cancer
    6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.
  • HY-15249
    JZL 184

    		MAGL Neurological Disease
    JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.
  • HY-13632
    Exemestane

    FCE 24304; EXE

    		 Cytochrome P450 Cancer Endocrinology
    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.
  • HY-P1407
    Z-VRPR-FMK TFA

    VRPR

    		 MALT1 Influenza Virus Cancer Infection
    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-12305
    Q-VD-OPh

    QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone

    		 Caspase HIV Cancer Infection
    Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
  • HY-135815A
    Mobocertinib succinate

    TAK-788 succinate; AP32788 succinate

    		 EGFR Cancer
    Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.
  • HY-B1496
    Tranylcypromine hemisulfate

    SKF 385 hemisulfate

    		 Monoamine Oxidase Histone Demethylase Neurological Disease
    Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
  • HY-17447SA
    Tranylcypromine-d5 hydrochloride

    SKF 385-d5 (hydrochloride)

    		 Monoamine Oxidase Histone Demethylase Neurological Disease
    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-B0334AS
    Sulbactam-d5 sodium

    		Bacterial Antibiotic Infection
    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-13272S3
    Dacomitinib-d10

    PF-00299804-d10; PF-299804-d10

    		 EGFR Apoptosis Cancer
    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-14872
    Tideglusib

    NP031112

    		 GSK-3 Neurological Disease
    Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
  • HY-P1010A
    Z-LEHD-FMK TFA

    		Caspase Apoptosis Cancer Neurological Disease
    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-13272S2
    Dacomitinib-d10 dihydrochloride

    PF-00299804-d10 (dihydrochloride); PF-299804-d10 (dihydrochloride)

    		 EGFR Apoptosis Cancer
    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-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-32721S
    Neratinib-d6

    		EGFR Cancer
    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-118284
    Vicagrel

    		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-79077
    Osimertinib dimesylate

    AZD-9291 dimesylate; Mereletinib dimesylate

    		 EGFR Cancer
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
  • HY-B2145
    Ilaprazole sodium

    IY-81149 sodium

    		 Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-P0034
    Ac-DEVD-CMK

    Caspase-3 Inhibitor III

    		 Caspase Apoptosis Metabolic Disease
    Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis.
  • HY-70013S
    Abiraterone-D4

    CB-7598-d4

    		 Cytochrome P450 Cancer
    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-144288
    BLK-IN-2

    		Btk Cancer
    BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC50 of 5.9 nM. BLK-IN-2 also inhibits BTK (IC50=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells.
  • 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-B0656
    Rabeprazole

    LY307640

    		 Proton Pump Apoptosis Bacterial Cancer Inflammation/Immunology
    Rabeprazole (LY307640) 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.
  • HY-B0656A
    Rabeprazole sodium

    LY307640 sodium

    		 Proton Pump Apoptosis Bacterial Inflammation/Immunology Cancer
    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.
  • 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-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-107411
    Bromoenol lactone

    (6E)-Bromoenol lactone

    		 Phospholipase Inflammation/Immunology
    Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx.
  • HY-19564
    JX06

    		PDHK Apoptosis Cancer
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
  • HY-D0843
    N-Ethylmaleimide

    NEM

    		 Cathepsin Deubiquitinase Apoptosis Others
    N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.
  • HY-13896
    PD168393

    		EGFR Autophagy Apoptosis Cancer
    PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
  • HY-P0034A
    Ac-DEVD-CMK TFA

    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-101664
    Ilaprazole

    IY-81149

    		 Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-14654
    Aspirin

    Acetylsalicylic Acid; ASA

    		 COX Virus Protease NF-κB Autophagy Apoptosis Mitophagy Caspase p38 MAPK Cancer Infection Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    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-114277
    Sotorasib

    AMG-510

    		 Ras Cancer
    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 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-109169B
    Bomedemstat hydrochloride

    IMG-7289 hydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
  • HY-129390
    Orelabrutinib

    ICP-022

    		 Btk Cancer
    Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
  • HY-10197
    Wortmannin

    SL-2052; KY-12420

    		 PI3K Polo-like Kinase (PLK) Autophagy Antibiotic Cancer
    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
  • HY-109169C
    Bomedemstat dihydrochloride

    IMG-7289 dihydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
  • 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.
  • HY-14380
    PF-3845

    		FAAH Autophagy Inflammation/Immunology Cancer
    PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
  • 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-109169
    Bomedemstat

    IMG-7289

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
  • HY-B0470
    Neomycin sulfate

    		Bacterial Antibiotic Phospholipase Infection
    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-10533
    Eniluracil

    5-Ethynyluracil; GW776C85

    		 Others Cancer
    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).
  • HY-13036C
    (Rac)-IBT6A hydrochloride

    		Btk Cancer
    (Rac)-IBT6A hydrochloride is a racemate of IBT6A hydrochloride. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-13036
    (Rac)-IBT6A

    		Btk Cancer
    (Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-B0334AS1
    Sulbactam-d2 sodium

    CP45899-d2 sodium

    		 Bacterial Antibiotic Infection
    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-122635A
    T-448

    		Histone Demethylase Neurological Disease
    T-448 is a specific, orally active 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-145928
    Divarasib

    GDC-6036

    		 Ras Cancer
    Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
  • HY-13822
    SKI II

    		SphK Wnt Apoptosis Cancer
    SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.
  • 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-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-15771
    Tirabrutinib

    ONO-4059; GS-4059

    		 Btk Apoptosis Cancer Inflammation/Immunology
    Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
  • HY-139920A
    Oritinib mesylate

    SH-1028 mesylate

    		 EGFR Cancer
    Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
  • HY-15771A
    Tirabrutinib hydrochloride

    ONO-4059 hydrochloride; GS-4059 hydrochloride

    		 Btk Apoptosis Cancer Inflammation/Immunology
    Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.
  • HY-129476
    L-Canaline

    		Parasite Endogenous Metabolite Cancer Infection
    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-15772A
    Osimertinib mesylate

    AZD-9291 mesylate; Mereletinib mesylate

    		 EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) 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.
  • HY-17600
    Acalabrutinib

    ACP-196

    		 Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-101560
    Linrodostat

    BMS-986205; ONO-7701

    		 Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers.
  • HY-14654A
    Aspirin lithium

    Acetylsalicylic Acid lithium; ASA lithium

    		 COX Virus Protease NF-κB Autophagy Apoptosis Mitophagy Caspase p38 MAPK Cancer Infection Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    Aspirin (Acetylsalicylic Acid) lithium 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 lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
  • HY-116423A
    JH295 hydrate

    		Others Cancer
    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.
  • HY-10985
    Marizomib

    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-106161
    Rupintrivir

    AG7088

    		 Virus Protease Enterovirus Infection Inflammation/Immunology
    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-B0033S
    Vigabatrin-13C,d2 hydrochloride

    γ-Vinyl-GABA-13C,d2 (hydrochloride)

    		 GABA Receptor Neurological Disease
    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-B0656S
    Rabeprazole-d4

    LY307640-d4

    		 Proton Pump Apoptosis Cancer Inflammation/Immunology
    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-15772
    Osimertinib

    AZD-9291; Mereletinib

    		 EGFR Cancer
    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. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-17447A
    Tranylcypromine hydrochloride

    SKF 385 hydrochloride

    		 Monoamine Oxidase Neurological Disease
    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-116423
    JH295

    		Others Cancer
    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.
  • HY-109169A
    Bomedemstat ditosylate

    IMG-7289 ditosylate

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
  • 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-N6775
    Sonolisib

    PX-866

    		 PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-13632S
    Exemestane-d2

    FCE 24304-d2; EXE-d2

    		 Cytochrome P450 Isotope-Labeled Compounds Cancer Endocrinology
    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-13632S2
    Exemestane-d3

    FCE 24304-d3; EXE-d3

    		 Cytochrome P450 Isotope-Labeled Compounds Cancer Endocrinology
    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-110130
    RN-1 dihydrochloride

    		Histone Demethylase Cancer Cardiovascular Disease
    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-139481
    TL-895

    		Btk Cancer Infection
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research.
  • HY-106376A
    L-Buthionine-(S,R)-sulfoximine

    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-10261S1
    Afatinib-d4

    BIBW 2992-d4

    		 EGFR Autophagy Cancer
    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-114436S
    MRTX-1257-d6

    MRTX-1257-d6

    		 Isotope-Labeled Compounds Cancer
    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-100433
    PACMA 31

    		PDI Cancer
    PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
  • HY-18977
    KML29

    		MAGL Metabolic Disease Inflammation/Immunology
    KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
  • HY-13632S1
    Exemestane-13C3

    		Cytochrome P450 Isotope-Labeled Compounds Cancer Endocrinology
    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-15888
    PTC-209

    		Autophagy Cancer
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-119033
    MGL-IN-1

    		MAGL Inflammation/Immunology
    MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant.
  • HY-122635
    T-448 free base

    		Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
  • HY-P0111
    Z-WEHD-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.
  • HY-133780
    Afatinib impurity 11

    		EGFR Autophagy Cancer
    Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-Z0816
    Dehydronitrosonisoldipine

    		Calcium Channel Others
    Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
  • HY-116090
    Conoidin A

    		Parasite Infection Neurological Disease Cardiovascular Disease
    Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
  • HY-12276
    MALT1 inhibitor MI-2

    		MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-B0656AS
    Rabeprazole-d4 sodium

    LY307640-d4 sodium

    		 Proton Pump Apoptosis Inflammation/Immunology Cancer
    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-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-124069
    M-525

    		Epigenetic Reader Domain Cancer
    M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.
  • HY-109189
    Rezivertinib

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-146390
    Antiproliferative agent-5

    		Autophagy Reactive Oxygen Species Cancer
    Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer.
  • HY-130242
    PXS-5120A

    		Monoamine Oxidase Inflammation/Immunology
    PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).
  • HY-15772S1
    Osimertinib-13C,d3

    AZD-9291-13C,d3; Mereletinib-13C,d3

    		 EGFR Cancer
    Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
  • HY-15772S
    Osimertinib-d6

    AZD-9291-d6; Mereletinib-d6

    		 EGFR Cancer
    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

    LY307640-d3 sodium

    		 Proton Pump Apoptosis Inflammation/Immunology Cancer
    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-13821
    Epoxomicin

    BU-4061T

    		 Proteasome Apoptosis Cancer Inflammation/Immunology
    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-W016420
    Fosfomycin sodium

    MK-0955 sodium

    		 Bacterial Antibiotic Infection Cancer
    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-139504
    CC-99677

    		MAPKAPK2 (MK2) Inflammation/Immunology
    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). CC-99677 is extracted from patent WO2020236636, compound 1.
  • HY-A0061S
    Trifluridine-13C,15N2

    Trifluorothymidine-13C,15N2; 5-Trifluorothymidine-13C,15N2; TFT-13C,15N2

    		 Thymidylate Synthase Nucleoside Antimetabolite/Analog HSV Orthopoxvirus Cancer
    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-116451
    PF-04859989 hydrochloride

    		Others Neurological Disease
    PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively).
  • HY-15888A
    PTC-209 hydrobromide

    		Autophagy Cancer
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-106376C
    L-Buthionine-(S,R)-sulfoximine hydrochloride

    L-Buthionine sulfoximine hydrochloride; L-BSO hydrochloride

    		 Ferroptosis Cancer Metabolic Disease
    L-Buthionine-(S,R)-sulfoximine hydrochloride is a cell-permeable, potent, fast acting, orally active 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-B1075A
    Fosfomycin

    MK-0955

    		 Bacterial Antibiotic Infection
    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-10261AS
    Afatinib-d6 dimaleate

    BIBW 2992MA2-d6

    		 EGFR Autophagy Cancer
    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-A0004
    Decitabine

    5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

    		 DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
  • HY-B1075
    Fosfomycin calcium

    MK-​0955 calcium

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium 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-B0609
    Fosfomycin tromethamine

    MK-0955 tromethamine

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine 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-117833
    PXS-4681A

    		Monoamine Oxidase Inflammation/Immunology
    PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.
  • HY-123931
    ZLDI-8

    		Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-147994
    EGFR/HER2-IN-5

    		EGFR Cancer
    EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.
  • HY-103387
    DuP-697

    		COX Apoptosis Cancer Inflammation/Immunology
    DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
  • HY-147992
    EGFR/HER2-IN-4

    		EGFR Cancer
    EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.
  • HY-146727
    JAK3-IN-11

    		JAK Inflammation/Immunology
    JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.
  • HY-12680
    PRN694

    		Itk Inflammation/Immunology
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
  • HY-135334
    ACP-5862

    		Drug Metabolite Btk Cytochrome P450 Cancer
    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.
  • 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-19985A
    (3S,4S)-PF-06459988

    		EGFR Cancer
    (3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    		 Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-112776
    BN82002

    		Phosphatase Cancer
    BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.
  • HY-112776A
    BN82002 hydrochloride

    		Phosphatase Cancer
    BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    		EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-17447AS
    (1S,2R)-Tranylcypromine-d5 hydrochloride

    (1S,2R)-SKF 385-d5 hydrochloride

    		 Monoamine Oxidase Neurological Disease
    (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].
  • HY-13207
    ONX-0914

    PR-957

    		 Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
  • HY-108467
    GGsTop

    Nahlsgen

    		 Others Cardiovascular Disease
    GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
  • HY-12972
    Mavelertinib

    PF-06747775

    		 EGFR Cancer
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
  • HY-17499
    EGFR-IN-12

    		EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-19617B
    EGFR-IN-1 TFA

    		EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-19617
    EGFR-IN-1

    		EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-13207A
    ONX-0914 TFA

    PR-957 TFA

    		 Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    		 IKK Deubiquitinase Autophagy Apoptosis NF-κB Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-B1075AS
    (Rac)-Fosfomycin (benzylamine)-13C3

    MK-0955 (benzylamine)-13C3

    		 Bacterial Antibiotic Infection
    (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-100848
    TX1-85-1

    		EGFR Cancer
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
  • HY-109010
    Poseltinib

    HM71224; LY3337641

    		 Btk BMX Kinase Toll-like Receptor (TLR) Metabolic Disease
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-W002585
    O6-Benzylguanine

    		DNA/RNA Synthesis Apoptosis Cancer
    O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
  • 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 Kds 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-151499
    PXS-6302

    		Monoamine Oxidase Others
    PXS-6302 is an irreversible lysyl oxidase inhibitor with IC50s of 3.7 μM (Bovine LOX), 3.4 μM (rh LOXL1), 0.4 μM (rh LOXL2), 1.5 μM (rh LOXL3), 0.3 μM (rh LOXL4), respectively. PXS-6302 has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance.
  • HY-125269
    TED-347

    		YAP Cancer
    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
  • HY-118529
    JUN-1111

    		Phosphatase Cancer
    JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1.
  • HY-123823
    Nitroaspirin

    NCX 4016

    		 COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-151201
    Steroid sulfatase/17β-HSD1-IN-3

    		Others Cancer
    Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-3 irreversibly inhibits hSTS activity with anIC50 value of 27 nM. Steroid sulfatase/17β-HSD1-IN-3 can be used in the study of endometriosis and other estrogen-dependent diseases.
  • HY-151202
    Steroid sulfatase/17β-HSD1-IN-4

    		Others Cancer
    Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity with anIC50 value of 63 nM. Steroid sulfatase/17β-HSD1-IN-4 can be used in the study of endometriosis and other estrogen-dependent diseases.
  • HY-100034
    NSC 663284

    DA-3003-1

    		 Phosphatase Histone Methyltransferase Cancer
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
  • HY-100818
    Futibatinib

    TAS-120

    		 FGFR Cancer
    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).
  • HY-146314
    MAO-B-IN-9

    		Monoamine Oxidase Amyloid-β Neurological Disease
    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 Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects.
  • HY-111553
    TAS0728

    		EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors.
  • HY-135334S
    ACP-5862-d4

    		Drug Metabolite Btk Cytochrome P450 Cancer
    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-131036
    MAO-IN-M30 dihydrochloride

    		Monoamine Oxidase Neurological Disease
    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.
  • HY-146677
    5-HT6R/MAO-B modulator 1

    		5-HT Receptor Monoamine Oxidase Neurological Disease
    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.
  • HY-N0110
    Palmatine chloride

    		Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    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-N0110A
    Palmatine

    		Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Palmatine 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.
  • HY-10261A
    Afatinib dimaleate

    BIBW 2992MA2

    		 EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK Cancer
    Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
  • HY-10261
    Afatinib

    BIBW 2992

    		 EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK Cancer
    Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
  • HY-10261D
    Afatinib oxalate

    BIBW 2992 oxalate

    		 EGFR Autophagy Apoptosis c-Met/HGFR Akt Cancer
    Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
  • HY-108137
    Z-LVG-CHN2

    		Cathepsin HSV SARS-CoV Infection Inflammation/Immunology
    Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease.
  • HY-111545
    BSc5371

    		FLT3 Cancer
    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines.
  • HY-N0110B
    Palmatine hydroxide

    		Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    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-101257B
    YKL-5-124 TFA

    		CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    		CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-108357
    6-Diazo-5-oxo-L-nor-Leucine

    L-6-Diazo-5-oxonorleucine; DON

    		 Glutaminase Bacterial Influenza Virus Antibiotic Cancer Infection
    6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity.
  • HY-N1638
    1-Methyl-2-undecyl-4(1H)-quinolone

    		Monoamine Oxidase Neurological Disease
    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 Ki 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-139920
    Oritinib

    SH-1028

    		 EGFR Cancer
    Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT, EGFR L858R, EGFR L861Q, EGFR L858R/T790M, EGFR d746-750 and EGFR d746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
  • HY-112823
    Almonertinib

    HS-10296

    		 EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    		 EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-113953
    Z-Asp-CH2-DCB

    		Caspase Apoptosis Inflammation/Immunology
    Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
  • HY-150510
    MS8511

    		Histone Methyltransferase Cancer Neurological Disease
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
  • HY-10261E
    (R)-Afatinib

    (R)-BIBW 2992

    		 EGFR c-Met/HGFR p38 MAPK Cancer
    (R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
  • HY-101522
    CHMFL-EGFR-202

    		EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.