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FKBP

FKBP ligands bind FK506-binding proteins (FKBPs), a family of peptidyl-prolyl cis-trans isomerases. In 1989 the receptor for the immunosuppressant FK506 (tacrolimus) was shown to be such an isomerase, now known as FKBP12. Pimecrolimus is a related macrolactam that also binds FKBP12 and inhibits calcineurin. SAFit1 and SAFit2 selectively inhibit FKBP51 through an induced-fit binding mode reported in 2015. Shield-1 stabilizes fusions to a destabilized FKBP12 domain, a method described in 2006 for rapid, reversible control of protein levels. AP1867 binds the engineered mutant FKBP12(F36V), and FKBP12 PROTAC dTAG-7 uses this ligand to degrade tagged proteins in the degradation tag (dTAG) system. Rimiducid and zapalog are chemical inducers of dimerization for FKBP fusion proteins.

3 Items

  • ILS-920
    Cat. No.
    A40919
    CAS No.
    892494-07-4

    ILS-920

    ILS-920 is an immunosuppressive modulator and a nonimmunosuppressive analog of Rapamycin, designed to exhibit reduced immunosuppressive effects while retaining neuroprotective properties. It selectively binds to FKBP52 and the β1-subunit of L-type voltage-gated calcium channels (VGCC), demonstrating a remarkable 200-fold selectivity for FKBP52 over FKBP12. This compound is of particular interest in research areas focusing on neuroprotection and the modulation of calcium signaling pathways.

    In stock View Details
    5 mg
    $255.00
    10 mg
    $405.00
    All 4 sizes
  • MP-010
    Cat. No.
    A40930
    CAS No.
    3024617-59-9

    MP-010

    MP-010 is a potent FKBP12 ligand that modulates cytosolic calcium levels by stabilizing ryanodine receptor (RyR) channel activity. This compound has been shown to enhance functional outcomes in SOD1G93A amyotrophic lateral sclerosis (ALS) mouse models, evidenced by improved motor coordination, enhanced integrity of neuromuscular junctions, and increased survival of spinal motor neurons. MP-010 serves as a valuable tool in the investigation of neurological disorders and the underlying mechanisms of ALS.

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    Out of stock

    All 3 sizes

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