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Results for "

Irreversible

" in MedChemExpress (MCE) Product Catalog:

866

Inhibitors & Agonists

5

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13

Fluorescent Dye

17

Biochemical Assay Reagents

31

Peptides

1

Inhibitory Antibodies

53

Natural
Products

64

Isotope-Labeled Compounds

29

Click Chemistry

2

Oligonucleotides

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1368
    Fenclonine
    20+ Cited Publications

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

    		 Tryptophan Hydroxylase Neurological Disease Cancer
    Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research .
    Fenclonine
  • HY-50202A
    Etomoxir sodium salt
    125+ Cited Publications

    (R)-(+)-Etomoxir sodium salt

    		 Carnitine Palmitoyltransferase (CPT) Apoptosis Metabolic Disease Cancer
    Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig .
    Etomoxir sodium salt
  • HY-17600
    Acalabrutinib
    30+ Cited Publications

    Calquence; ACP-196

    		 Btk Inflammation/Immunology 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). Acalabrutinib can be used for CLL research . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib
  • HY-147250
    Lirafugratinib
    1 Publications Verification

    RLY-4008

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib
  • HY-141680
    CPS2
    1 Publications Verification

    		 PROTACs CDK Cancer
    CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia .
    CPS2
  • HY-164388
    Z-VAD
    Maximum Cited Publications
    19 Publications Verification

    		 Caspase Apoptosis Autophagy Necroptosis Cardiovascular Disease Cancer
    Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
    Z-VAD
  • HY-10985
    Marizomib
    15+ Cited Publications

    Salinosporamide A; NPI-0052

    		 Proteasome Cancer
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively) .
    Marizomib
  • HY-101257
    YKL-5-124
    15+ Cited Publications

    		 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 .
    YKL-5-124
  • HY-103334
    MAFP
    5 Publications Verification

    Methyl Arachidonyl Fluorophosphonate

    		 Phospholipase Cardiovascular Disease Neurological Disease Metabolic Disease
    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
    MAFP
  • HY-B0334
    Sulbactam
    10+ Cited Publications

    CP45899

    		 Bacterial Antibiotic Infection
    Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
    Sulbactam
  • 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 .
    NU6300
  • HY-B0334A
    Sulbactam sodium
    10+ Cited Publications

    CP45899 sodium

    		 Bacterial Antibiotic Infection
    Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
    Sulbactam sodium
  • HY-115673
    LAS17
    1 Publications Verification

    		 Glutathione S-transferase Cancer
    LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM . LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LAS17
  • HY-125269
    TED-347
    10+ Cited Publications

    		 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 .
    TED-347
  • HY-147250A
    Lirafugratinib hydrochloride
    1 Publications Verification

    RLY-4008 hydrochloride

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib hydrochloride
  • HY-114436
    MRTX-1257
    5 Publications Verification

    		 Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257
  • HY-W017423
    (-)-Carvone

    		Environmental Pollutants 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 .
    (-)-Carvone
  • HY-139504
    Gamcemetinib

    CC-99677

    		 MAPKAPK2 (MK2) Inflammation/Immunology
    Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
    Gamcemetinib
  • HY-124628
    IPI-9119
    2 Publications Verification

    		 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 .
    IPI-9119
  • HY-112274
    M443
    3 Publications Verification

    		 Mixed Lineage Kinase Cancer
    M443 is an irreversible and specific inhibitor of MRK, with an IC50<125 nM.
    M443
  • HY-13427
    Allitinib tosylate
    2 Publications Verification

    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
    Allitinib tosylate
  • HY-115733
    Cathepsin L-IN-2
    1 Publications Verification

    (Rac)-Z-Phe-Phe-FMK

    		 Cathepsin Cancer
    Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) is an isomer of the Cathepsin L inhibitor Z-Phe-Phe-FMK (HY-141867), with an IC50 of 15 μM for cathepsin L. Z-Phe-Phe-FMK irreversibly blocks the proteolytic function of cathepsins by covalently binding to the cysteine residues in the active center of the enzyme. Cathepsin L-IN-2 and Z-Phe-Phe-FMK can be used to study neurodegenerative diseases (such as GRN-related frontotemporal dementia) and cancer invasion and metastasis.
    Cathepsin L-IN-2
  • 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 .
    PF-06459988
  • HY-P0034
    Ac-DEVD-CMK
    3 Publications Verification

    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 Ingenol 3,20-dibenzoate?(HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis .
    Ac-DEVD-CMK
  • HY-109143
    Elsubrutinib
    2 Publications Verification

    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 .
    Elsubrutinib
  • HY-Z0816
    Dehydronitrosonisoldipine
    3 Publications Verification

    		 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 .
    Dehydronitrosonisoldipine
  • 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) .
    Mofegiline hydrochloride
  • HY-112823A
    Almonertinib mesylate
    5+ Cited Publications

    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 .
    Almonertinib mesylate
  • HY-101868
    INF39
    10+ Cited Publications

    		 NOD-like Receptor (NLR) Inflammation/Immunology
    INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.
    INF39
  • HY-15375
    Allitinib
    2 Publications Verification

    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 .
    Allitinib
  • HY-136605
    DGY-06-116
    2 Publications Verification

    		 Src Cancer
    DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM .
    DGY-06-116
  • HY-W019847
    Azamulin

    		Cytochrome P450 Infection Metabolic Disease
    Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .
    Azamulin
  • HY-P0034A
    Ac-DEVD-CMK TFA
    3 Publications Verification

    Caspase-3 Inhibitor III TFA

    		 Caspase Apoptosis Metabolic Disease
    Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK TFA significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK TFA can be used in a variety of experimental approaches to inhibit apoptosis .
    Ac-DEVD-CMK TFA
  • HY-141677
    INCB059872

    		Histone Demethylase Cancer
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 can be used for the research of myeloid leukemia .
    INCB059872
  • HY-132817
    Gunagratinib
    1 Publications Verification

    ICP-192

    		 FGFR Cancer
    Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer . Gunagratinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
    Gunagratinib
  • HY-110130
    RN-1 dihydrochloride

    		Histone Demethylase Cardiovascular Disease Cancer
    RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively .
    RN-1 dihydrochloride
  • 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 .
    FIIN-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) .
    Menin-MLL inhibitor 20
  • 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 .
    GSK-2793660
  • HY-W143698
    PDGFRα kinase inhibitor 2

    		Bcr-Abl c-Kit PDGFR Cancer
    PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
    PDGFRα kinase inhibitor 2
  • 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 .
    MPO-IN-1
  • HY-101257B
    YKL-5-124 TFA
    15+ Cited Publications

    		 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 .
    YKL-5-124 TFA
  • HY-17600S
    Acalabrutinib-d4

    ACP-196-d4

    		 Btk Cancer
    Acalabrutinib-d4 (ACP-196-d4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib-d4
  • HY-139920
    Oritinib
    1 Publications Verification

    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 .
    Oritinib
  • HY-143319
    SPH5030

    		EGFR 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 .
    SPH5030
  • HY-141677A
    INCB059872 dihydrochloride

    		Histone Demethylase Cancer
    INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 dihydrochloride can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .
    INCB059872 dihydrochloride
  • HY-W796158
    Z-DEVD-CMK

    		Cathepsin Inflammation/Immunology
    Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro .
    Z-DEVD-CMK
  • HY-164725
    FAPI-mFS

    		Radionuclide-Drug Conjugates (RDCs) FAP Cancer
    FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu . FAPI-mFS can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    FAPI-mFS
  • HY-W772850
    Fenclonine hydrochloride
    20+ Cited Publications

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

    		 Tryptophan Hydroxylase Neurological Disease Cancer
    Fenclonine hydrochloride is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine hydrochloride can be used in carcinoid syndrome research .
    Fenclonine hydrochloride
  • HY-106582
    Sobuzoxane

    MST 16

    		 Topoisomerase Neurological Disease Cancer
    Sobuzoxane (MST-16) is an orally active topoisomerase II inhibitor. Sobuzoxane causes irreversible inhibition of cell division. Sobuzoxane can be used in the study of non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has recurred .
    Sobuzoxane

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