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mTOR

Mechanistic target of rapamycin (mTOR) inhibitors act on a kinase that links nutrient signals to cell growth. In 1994 mTOR was identified as the mammalian protein targeted by rapamycin bound to its receptor. The kinase forms a nutrient-sensitive complex with raptor, known as mTOR complex 1 (mTORC1), and a second complex, mTOR complex 2 (mTORC2). Sirolimus and its derivative everolimus act through FK506-binding protein 12 (FKBP12) and mainly inhibit mTORC1. Catalytic-site inhibitors such as Torin 1 and AZD8055 block both complexes. With Torin 1, rapamycin-resistant functions of mTORC1 were revealed in 2009. Dual phosphoinositide 3-kinase (PI3K)/mTOR inhibitors such as dactolisib are also listed here.

2 Items

  • PD-M6
    Cat. No.
    A79733
    CAS No.
    3058330-82-5

    PD-M6

    PD-M6 is an mTOR-targeted PROTAC degrader that facilitates the ubiquitination and subsequent degradation of mTOR, exhibiting a DC50 of 4.8 μM. This compound has demonstrated potent anti-proliferative effects on HeLa, MCF-7, and HepG2 cancer cell lines, with IC50 values of 11.3, 2.58, and 3.23 μM, respectively. Additionally, PD-M6 induces autophagy and specifically promotes the degradation of LAMTOR1, a pivotal component of the mTOR signaling pathway, suggesting its utility for investigating mTOR-related biological processes in cancer research.

    In stock View Details
    5 mg
    $210.00
    10 mg
    $340.00
    All 5 sizes
  • YB-3–17
    Cat. No.
    A79743
    CAS No.
    2940242-88-4

    YB-3–17

    YB-3-17 is a bifunctional PROTAC molecule that targets the mechanistic target of rapamycin (mTOR) with an IC50 of 0.22 nM and induces degradation of G1 to S phase transition 1 gene (GSPT1) with a DC50 of 5 nM. This compound demonstrates significant antiproliferative effects in various glioblastoma cell lines, achieving nanomolar IC50 values. Additionally, YB-3-17 exhibits notable antitumor efficacy in preclinical mouse models, making it a valuable tool for studying mTOR inhibition and its implications in cancer therapy.

    In stock View Details
    5 mg
    $155.00
    10 mg
    $240.00
    All 5 sizes

2 Items

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