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Results for "

GNE987

" in MedChemExpress (MCE) Product Catalog:

5

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129937A
    GNE-987

    		PROTACs Epigenetic Reader Domain Cancer
    GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
    <em>GNE-987</em>
  • HY-129939
    PROTAC BRD4 ligand-1

    		Epigenetic Reader Domain Ligands for Target Protein for PROTAC Cancer
    PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A) .
    PROTAC BRD4 ligand-1
  • HY-129938
    PROTAC BRD4 Degrader-24

    		PROTAC-Linker Conjugates for PAC Cancer
    PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker .
    PROTAC BRD4 Degrader-24
  • HY-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3

    		PROTAC-Linker Conjugates for PAC ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 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.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-129937
    (S)-GNE-987

    		PROTACs Epigenetic Reader Domain Cancer
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
    (S)-<em>GNE-987</em>

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