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Smoothened Receptors

Smoothened receptor agonists and antagonists bind Smoothened (SMO), the transducer of Hedgehog signals. The Drosophila smoothened gene was shown in 1996 to encode a seven-pass membrane protein, first proposed as a Hedgehog receptor. SMO is now grouped with class F G protein-coupled receptors (GPCRs). In 2002 the Veratrum alkaloid cyclopamine was found to bind the SMO heptahelical bundle directly. A study the same year identified the synthetic agonist SAG as a direct SMO ligand. Sonidegib, glasdegib and taladegib are SMO antagonists, and saridegib is a semisynthetic cyclopamine analog. Jervine, a related Veratrum alkaloid, also inhibits SMO, while the glucocorticoid halcinonide is listed as an SMO agonist.

1 Item

  • BODIPY-Cyclopamine
    Cat. No.
    A84827
    CAS No.
    334658-24-1

    BODIPY-Cyclopamine

    BODIPY-Cyclopamine is a fluorescent ligand targeting the Smoothened (SMO) receptor, crucial for Hedgehog signaling pathway regulation. Dysregulation of this pathway is linked to tumorigenesis, making BODIPY-Cyclopamine valuable for research related to cancer biology. Utilizing the NanoBRET (Nanofluorescein bioluminescence resonance energy transfer) technique, this compound facilitates the sensitive detection of energy transfer between SMO and the fluorescent probe, enabling high-throughput screening and kinetic studies. Additionally, investigating the binding dynamics of BODIPY-Cyclopamine can assist in the development of SMO-targeted therapeutics.

    In stock View Details
    0.25 mg
    $435.00
    0.5 mg
    $750.00
    All 6 sizes

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