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bivalent degrader

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153119

    Ligands for Target Protein for PROTAC Others
    TMX-4153 is a bivalent degrader. TMX-4153 rapidly and selectively degrades endogenous PIP4K2C by recruiting the von Hippel-Lindau (VHL) E3 ligase complex, with a KD value of 42 nM. TMX-4153 can be used to synthesize PROTAC .
    TMX-4153
  • HY-122702

    PROTAC Linkers Others
    PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation .
    PEG6-(CH2CO2H)2
  • HY-125593

    APG-1387

    IAP Apoptosis Cancer
    Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma .
    Dasminapant
  • HY-16591
    Birinapant
    25+ Cited Publications

    TL32711

    IAP Apoptosis HIV Cancer
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
    Birinapant
  • HY-160528

    Epigenetic Reader Domain Molecular Glues Cancer
    IBG3 is a dual-JQ1-containing BET degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
    IBG3
  • HY-118998

    EGFR Cancer
    TX2-121-1, a potent and selective Her3 (ErbB3) bivalent ligand, can induce degradation of Her3 with an IC50 of 49 nM. TX2-121-1 can inhibit Her3-dependent signaling .
    TX2-121-1
  • HY-125001

    Others Others
    JH-VIII-49 is a potent and selective CDK8 inhibitor with excellent biological activity. The synthesis of JH-VIII-49 is simplified to eight steps with an overall yield of 33%, making it suitable for large-scale production. JH-VIII-49 promotes CDK8 inhibition through its steroid skeleton design. JH-VIII-49 provides a basis for the subsequent development of more complex bivalent small molecule degraders .
    JH-VIII-49
  • HY-130711

    VH032-C3-NH2

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
    (S,R,S)-AHPC-C3-NH2
  • HY-130711A

    VH032-C3-NH2 TFA

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
    (S,R,S)-AHPC-C3-NH2 TFA
  • HY-130711C

    VH032-C3-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
    (S,R,S)-AHPC-C3-NH2 dihydrochloride

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