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sRANKL inhibitor S3-15

Chemical Structure : sRANKL inhibitor S3-15

CAS No.: 2412947-15-8

sRANKL inhibitor S3-15 (S3-15)

Catalog No.: PC-49334Not For Human Use, Lab Use Only.

sRANKL inhibitor S3-15 is a highly potent, orally active inhibitor of soluble RANKL, selectively interrupt soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction, shows potent osteoclast inhibition effect with IC50 of 0.19 uM in vitro.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    sRANKL inhibitor S3-15 is a highly potent, orally active inhibitor of soluble RANKL, selectively interrupt soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction, shows potent osteoclast inhibition effect with IC50 of 0.19 uM in vitro.
    S3-15 can bind to sRANKL at the enlarged stable region (binding site), and unable to bind to mRANKL at the shrunken stable region.
    S3-15 inhibits sRANKL induced osteoclast differentiation, while exhibits weak osteoclast differentiation in mRANKL induced osteoclastogenesis assay.
    S3-15 suppresses RANKL-induced NF-κB signaling by decreasing the phosphorylation of the IκB kinase-α (IKKα), NF-κB inhibitor-α (IκBα) and p65.
    S3-15 dose-dependently blocked both downstream transcription factor NF-κB and NFATC luciferase reporter-gene expression of RANKL-RANK signaling.
    S3-15 selectively inhibits sRANKL without changing T lymphocyte differentiation.
    S3-15 exhibits anti-osteoporotic effects without causing immunosuppression in ovariectomy (OVX) rats.

    Physicochemical Properties

    M.Wt 326.312
    Formula C16H14N4O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-[2-[2-Oxo-1-[(2-pyridinylamino)carbonyl]propylidene]hydrazinyl]benzoic acid

    References

    1. Huang D, et al. Nat Commun. 2022 Sep 12;13(1):5338.

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