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HSP

Heat shock protein (HSP) inhibitors, mostly HSP90 inhibitors, block chaperones that fold and stabilize client proteins. HSP90 binds and hydrolyzes adenosine triphosphate (ATP), and many of its clients are kinases and transcription factors in growth signaling. In 1994, benzoquinone ansamycins such as geldanamycin were shown to disrupt HSP90 complexes with the viral Src kinase. A crystal structure reported in 1997 placed geldanamycin in the N-terminal ATP pocket of HSP90. Inhibition leads to degradation of client proteins through the ubiquitin-proteasome pathway. Later chemotypes include the resorcinol-based luminespib and ganetespib, alongside the geldanamycin analog alvespimycin hydrochloride. JG-98 is an allosteric inhibitor of HSP70, a second chaperone family.

2 Items

  • PROTAC HSP90 degrader BP3
    Cat. No.
    A24714
    CAS No.
    2669072-88-0

    PROTAC HSP90 degrader BP3

    PROTAC HSP90 Degrader BP3 is a selective agent designed for targeted degradation of Heat Shock Protein 90 (HSP90) through a CRBN-dependent mechanism. This compound effectively degrades HSP90 in MCF-7 breast cancer cells, with a DC50 value of 0.99 µM, and demonstrates significant inhibition of cell growth. Additionally, BP3 features an alkyne group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool for advanced chemical biology applications.

    In stock View Details
    5 mg
    $535.00
    10 mg
    $855.00
    All 5 sizes
  • PROTAC Hsp90α degrader 1
    Cat. No.
    A37518
    CAS No.
    3031078-90-4

    PROTAC Hsp90α degrader 1

    PROTAC Hsp90α degrader 1 is a selective degrader targeting the heat shock protein 90 alpha (Hsp90α) through the PROTAC (proteolysis targeting chimeras) mechanism. This compound exhibits significant cytotoxic activity against various breast cancer cell lines, including MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM, respectively. PROTAC Hsp90α degrader 1 is valuable for investigating the role of Hsp90α in oncogenesis and developing targeted therapies for breast cancer.

    In stock View Details
    5 mg
    $330.00
    10 mg
    $545.00
    All 4 sizes

2 Items

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