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E3 Ligase Ligand-linker Conjugate 159

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-170827
    E3 Ligase Ligand-linker Conjugate 159

    		E3 Ligase Ligand-Linker Conjugates Cancer
    E3 Ligase Ligand-linker Conjugate 159 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 159 can be used for the synthesis of SMD-3236 (HY-170824), a PRAOTAC that targets the degradation of SMARCA2, exhibiting long-lasting antitumor activity in vivo .
    E3 Ligase Ligand-linker Conjugate 159
  • HY-170824
    SMD-3236

    		PROTACs Epigenetic Reader Domain Cancer
    SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
    SMD-3236

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