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Pathways Recommended: PROTAC
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PROTAC PI3Kδ degrader-1

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-176239
    PROTAC PI3Kδ degrader-1

    		PROTACs PI3K Akt Apoptosis Autophagy Cancer
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • HY-174461
    PROTAC PI3Kα degrader-1

    		PROTACs PI3K Cancer
    PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
    PROTAC PI3Kα degrader-1
  • HY-182083
    PROTAC PI3Kα/δ degrader-1

    		PROTACs PI3K Cancer
    PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer .
    PROTAC PI3Kα/δ degrader-1
  • HY-W937057
    (S,R,S)-AHPC-Me-10-bromodecanoic acid

    		E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate that incorporates a VHL ligand 2 (HY-112078) and linker 10-bromoheptanoic acid. (S,R,S)-AHPC-Me-10-bromodecanoic acid can be used for synthesis of PROTAC PI3Kδ degrader-1 (HY-176239) .
    (S,R,S)-AHPC-Me-10-bromodecanoic acid

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