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covalent ligand

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

4

Screening Libraries

1

Fluorescent Dye

2

Biochemical Assay Reagents

1

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2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-134761

    c-Myc Cancer
    EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis .
    EN4
  • HY-W229874

    E1/E2/E3 Enzyme Cancer
    EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1 .
    EN106
  • HY-153918A

    Ligands for Target Protein for PROTAC Cancer
    (S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control..
    (S)-SKBG-1
  • HY-151716

    PROTAC Linkers Others
    Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples .
    Halo-DBCO
  • HY-122577

    Aldehyde Dehydrogenase (ALDH) Cancer
    EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM
    EN40
  • 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-134184

    AUTACs Autophagy Inflammation/Immunology Cancer
    AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. SLF binds non-covalently to FKBP12 .
    AUTAC2
  • HY-115715

    E1/E2/E3 Enzyme Cancer
    EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination .
    EN219
  • HY-W1005067

    Molecular Glues Hippo (MST) Estrogen Receptor/ERR Others
    EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
    EN171
  • HY-150905

    EGFR Cancer
    EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
    EGFR ligand-2
  • HY-158301
    MY-1B
    1 Publications Verification

    DNA Methyltransferase Others
    MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .
    MY-1B
  • HY-141550

    NF-κB Inflammation/Immunology
    BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
    BPK-25
  • HY-161242

    Bcl-2 Family Cancer
    CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
    CBI1
  • HY-155075

    PROTACs Glutathione Peroxidase Ferroptosis Cancer
    NC-R17 is a PROTAC-class, non-covalent GPX4 degrader based on RSL3, involved in ferroptosis. NC-R17 has antitumor activity and is used for non-covalent GPX4 PROTAC design . NC-R17 consists of a target protein ligand (red part) Demethyl-RSL3 (HY-135832); an E3 ubiquitin ligase ligand (blue part) Lenalidomide (HY-A0003) and a PROTAC linker (black part) (HY-169376). E3 ubiquitin ligase and linker can form Lenalidomide-C13-piperazine-Boc (HY-169377) .
    NC-R17
  • HY-161242A

    Bcl-2 Family Cancer
    CBI1 formic is a covalent BAX inhibitor. CBI1 formic selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 formic blocks t-2-hex lipidation and oligomerization of BAX. CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
    CBI1 formic
  • HY-149933

    Cannabinoid Receptor Neurological Disease
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
    AM841
  • HY-144323

    PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
    YF135
  • HY-170453

    Epigenetic Reader Domain Cancer
    iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
    iHAC
  • HY-164389

    Ras Cancer
    SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
    SML-10-70-1
  • HY-122054

    Keap1-Nrf2 Cancer
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
    BPK-29
  • HY-122054A

    Keap1-Nrf2 Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
    BPK-29 hydrochloride
  • HY-153934

    GHR Endocrinology
    Tetrazole-C15-(N-acetylsulfamoyl)butanoic acid (Ligand 1) improves the pharmacokinetic properties of therapeutic peptides and proteins through non-covalent binding with human serum albumin (HSA). Tetrazole-C15-(N-acetylsulfamoyl)butanoic acid can be used for synthesis of long-acting human growth hormone (HGH) analog somapacitan .
    Tetrazole-C15-(N-acetylsulfamoyl)butanoic acid
  • HY-164977

    PROTACs Phosphatase Cancer
    JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3 ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .
    JCS-1
  • HY-167819

    Biochemical Assay Reagents
    D-Erythro-sphingosyl phosphoinositol is a lipid nanoparticle covalently linked to an antibody with potential activity in targeted compound delivery. D-Erythro-sphingosyl phosphoinositol can enhance the accumulation of compounds in specific cell types. D-Erythro-sphingosyl phosphoinositol may be used as a ligand to enhance the effect of antibodies in immunosuppression. D-Erythro-sphingosyl phosphoinositol can also be used to study the mechanisms related to cell signaling and lipid metabolism.
    D-Erythro-sphingosyl phosphoinositol
  • 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-158008

    Ras Cancer
    (R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .
    (R)-G12Di-7
  • HY-W145665

    Biochemical Assay Reagents Endogenous Metabolite Others
    Amylose is not a typical small-molecule ligand with a specific traditional receptor-binding target. It is a polysaccharide. In food science and biological systems, amylose can interact with proteins and free fatty acids through non-covalent forces like hydrophobic interactions and electrostatic interactions. For example, it can form a ternary complex with them, which is related to the structure and digestion of starch. It is widely studied in the fields of food science, carbohydrate metabolism, and is also relevant in research on controlling glycemic responses, as it affects starch digestion rate .
    Amylose
  • HY-129610

    PROTACs FKBP Cancer
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .
    KB02-SLF
  • HY-153357

    PROTACs Btk Cancer
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM) . NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex . NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).
    NRX-0492
  • HY-158036

    PROTACs STING Others Inflammation/Immunology
    PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
    PROTAC STING Degrader-2
  • HY-W394551

    Biochemical Assay Reagents Others
    Methyl 3,4-dibromo-2,5-dioxo-2,5-dihydro-1H-pyrrole-1-carboxylate is a small pyrrolidone molecule which features two bromine atoms and a methyl ester. The unsaturated dibromo motif is a covalent ligand for thiol groups, and may be used to label cysteine residues in proteins. The presence of two leaving groups on this molecule allows this linker to bind two thiols at a time. The methyl ester can be saponified to link this molecule to amines to form larger structures.
    Methyl 3,4-dibromo-2,5-dioxo-2,5-dihydro-1H-pyrrole-1-carboxylate
  • HY-115715A

    Fluorescent Dye Cancer
    EN219-alkyne is an alkyne-functionalized EN219 probe. EN219 (HY-P0287A) is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination . EN219-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EN219-alkyne
  • HY-129917
    KB02-JQ1
    4 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
    KB02-JQ1

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