1. Search Result
Search Result
Results for "

covalent binding

" in MedChemExpress (MCE) Product Catalog:

52

Inhibitors & Agonists

3

Screening Libraries

4

Fluorescent Dye

1

Biochemical Assay Reagents

1

Natural
Products

2

Isotope-Labeled Compounds

3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100739
    RA190
    3 Publications Verification

    Proteasome Cancer
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
    RA190
  • HY-U00447

    MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
    PK11000
  • HY-N12840

    Others Metabolic Disease
    Logmalicid B is an iridoid glycoside compound that can be isolated from Cornus officinalis and can be used in diabetes research .
    Logmalicid B
  • HY-126152

    Others Others
    Chlorthiamid is a broad-spectrum herbicide. Chlorthiamid is an olfactory toxicant with a high in vivo covalent binding in the olfactory mucosa of mice .
    Chlorthiamid
  • HY-133738

    Epigenetic Reader Domain Cancer
    M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM .
    M-808
  • HY-138065

    Apoptosis Others
    Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes .
    Iodoacetyl-LC-biotin
  • HY-120188

    PPAR Others
    CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
    CC618
  • HY-19564
    JX06
    1 Publications Verification

    PDHK Apoptosis Cancer
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity .
    JX06
  • HY-47573

    G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease Cancer
    CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .
    CCG273441
  • HY-117203A

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
    CDK12-IN-E9
  • HY-124645

    Flavivirus Dengue virus Btk MNK Infection Cancer
    QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies .
    QL-X-138
  • HY-D2270

    Fluorescent Dye Others
    Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and high affinity .
    Halo tag TMR
  • HY-155990

    RUNX-IN-1

    Apoptosis Cancer
    Chb-M′ (Compound Conjugate 1) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. Chb-M′ induces the p53-dependent apoptosis and inhibits cancer cell growth. Chb-M′ inhibits tumor growth in PANC-1 xenograft mice .
    Chb-M′
  • HY-138825

    Pyk2 Metabolic Disease
    NCGC00188636 is a novel covalent pyruvate kinase (PYK) inhibitor. NCGC00188636 blocks nucleotide binding to the active site of pyruvate kinase. NCGC00188636 can be used for the research of the metabolism of many organisms and cell types.
    NCGC00188636
  • HY-153728

    Histone Methyltransferase Cancer
    WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC. WM-586 specifically decreases cellular WDR5 and MYC interaction with the IC50 of 101 nM in HTRF assay .
    WM-586
  • HY-D2170

    Fluorescent Dye Others
    AF488 streptavidin is a fluorescence labeled streptavidin. AF488 streptavidin comprises a biotin-binding protein (streptavidin) covalently attached to a fluorescent label (AF488). AF488 is a bright, photostable green fluorophore .
    AF488 streptavidin
  • HY-103462

    FAAH Metabolic Disease Inflammation/Immunology Cancer
    TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders .
    TC-F2
  • HY-P3152
    Streptavidin
    1 Publications Verification

    Biochemical Assay Reagents Others
    Streptavidin is a ∼60 kDa homotetramer. Streptavidin binds four molecules of biotin with the highest affinity. The binding affinity of biotin to streptavidin is one of the highest reported for a non-covalent interaction to date, with a KD ∼ 0.01 pM . Streptavidin has an immunosuppressive role .
    Streptavidin
  • HY-149929

    Beta-lactamase Bacterial Infection
    EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7 .
    EBL-3183
  • HY-19706
    ARS-853
    2 Publications Verification

    Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
    ARS-853
  • HY-155991

    Apoptosis Cancer
    RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity .
    RUNX-IN-2
  • HY-105129A
    Pimonidazole
    4 Publications Verification

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor . Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
    Pimonidazole
  • HY-105129
    Pimonidazole hydrochloride
    4 Publications Verification

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor . Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
    Pimonidazole hydrochloride
  • HY-D0056

    Fluorescent Dye Others
    5-Carboxyfluorescein diacetate N-succinimidyl ester is a cell permeable dye (Ex=492 nm, Em=517 nm). 5-Carboxyfluorescein diacetate N-succinimidyl ester can label cells by covalently binding to intracellular molecules. 5-Carboxyfluorescein diacetate N-succinimidyl ester is used to track lymphocyte migration and proliferation .
    5-Carboxyfluorescein diacetate N-succinimidyl ester
  • HY-144650

    Apoptosis HSP Cancer
    Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90Cdc37 by covalent-binding, and induces apoptosis .
    Hsp90-Cdc37-IN-3
  • HY-108553

    Proteasome Apoptosis Cancer
    Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .
    Dihydroeponemycin
  • HY-103046

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent .
    UbcH5c-IN-1
  • HY-105129AS

    Isotope-Labeled Compounds Cancer
    Pimonidazole-d10 is the deuterium labeled Pimonidazole. Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor[1]. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia [2].
    Pimonidazole-d10
  • HY-151968

    Ras Cancer
    KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
    KRAS G12C inhibitor 57
  • HY-161066

    Ras Cancer
    KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS G13D (IC50: 0.41 nM). The selectivity for KRAS G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .
    KRAS G13D-IN-1
  • HY-138565
    K-975
    5+ Cited Publications

    YAP Cancer
    K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
    K-975
  • HY-132817

    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-129589

    ADC Cytotoxin Cancer
    Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC .
    Thailanstatin A
  • HY-W757743

    ACP-196-d3

    Isotope-Labeled Compounds Others
    Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
    Acalabrutinib-d3
  • HY-144605

    EGFR PROTACs Cancer
    PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
    PROTAC EGFR degrader 3
  • HY-15317
    RI-1
    4 Publications Verification

    RAD51 Cancer
    RI-1 is a RAD51 inhibitor, with IC50s ranging from 5 to 30 μM. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319. RI-1 inactivates RAD51 by directly binding to a protein surface that serves as an interface between protein subunits in RAD51 filaments. RI-1 can disrupt homologous recombination in human cells .
    RI-1
  • HY-162471

    Others Cancer
    GSK_WRN3 is a selective inhibitor of WRN protease (IC50 = 8.6 μM). GSK_WRN3 displays a high degree of selectivity by forming a covalent binding to the Cys727 residue of the WRN protein. GSK_WRN3 reduces growth support for MSI tumor cells by inhibiting WRN protease activity, resulting in increased DNA double-strand breaks and cell growth inhibition .
    GSK_WRN3
  • HY-100848
    TX1-85-1
    1 Publications Verification

    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 .
    TX1-85-1
  • HY-W760183

    Others Cancer
    EM12-SO2F is a powerful covalent inhibitor of CRBN through binding at His353. EM12-SO2F is a useful chemical probe to investigate the CRBN. EM12-SO2F inhibits the degradation of IKZF1 by lenalidomide (HY-A0003) in MOLT4 cells
    EM12-SO2F
  • HY-17600
    Acalabrutinib
    Maximum Cited Publications
    20 Publications Verification

    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) . 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-146727

    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 .
    JAK3-IN-11
  • HY-D1886

    Fluorescent Dye Others
    Vari Fluor 647 SE is a fluorescent dye, SE stands for "succinimidyl ester". Vari Fluor 647 SE belongs to the Vari Fluor family of labeling reagents used in cell and molecular biology research. Vari Fluor 647 SE can react with an amino group to form a covalent bond, thereby introducing Vari Fluor 647 dye into the target molecule or cell. Vari Fluor 647 SE is a reactive dye that produces a fluorescent signal after binding to a target molecule or cell.
    Vari Fluor 647 SE
  • HY-161579

    NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    NLRP3-IN-39 (Compound 49) inhibits the assembly and activation of NLRP3 inflammatory vesicles. NLRP3-IN-39 exerts its inhibitory effect by covalently binding to Cys 279 of the NLRP3 protein. NLRP3-IN-39 inhibits Nigericin (HY-127019)-induced IL-1β release from THP-1 cells (IC50= 0.29 μM) .
    NLRP3-IN-39
  • HY-111553

    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 BMXHER4BLK、EGFR、JAK3SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors .
    TAS0728
  • HY-158107

    Ras Cancer
    BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .
    BBO-8520
  • HY-161364

    Bacterial Inflammation/Immunology
    Antibacterial agent 200 (pyridyl HH 7), a unique hydrazyl hydroxycoumarin (HH), has strong antibacterial efficacy and broad antibacterial spectrum with MIC values ranging from 0.5 to 32 μg/mL for Gram-positive and Gram-negative bacteria. Antibacterial agent 200 exhibits a good inhibition against Pseudomonas aeruginosa 27853 with a low MIC value of 0.5 μg/mL. Antibacterial agent 200 can eradicate the integrity of bacterial membrane, result in the leakage of intracellular proteins, and interact with bacterial DNA gyrase via non-covalent binding .
    Antibacterial agent 200
  • HY-17600R

    Cancer
    Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. 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 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib (Standard)
  • HY-150510

    Histone Methyltransferase Neurological Disease Cancer
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and 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) .
    MS8511
  • HY-134318B

    DNA/RNA Synthesis Others
    8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    8-Azido-ADP disodium
  • HY-101522

    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 .
    CHMFL-EGFR-202

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

 

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

 

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: