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SK-124

Chemical Structure : SK-124

CAS No.: 2760404-50-8

SK-124 (SK124)

Catalog No.: PC-49563Not For Human Use, Lab Use Only.

SK-124 (SK124) is a potent, selective, orally active SIK2/SIK3 inhibitor with IC50 of 8.8/11.3 nM in cell-based NanoBRET assays, 15-fold selectivity versus SIK1.

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    Biological Activity

    SK-124 (SK124) is a potent, selective, orally active SIK2/SIK3 inhibitor with IC50 of 8.8/11.3 nM in cell-based NanoBRET assays, 15-fold selectivity versus SIK1.
    SK-124 potently inhibits SIK2/SIK3 with IC50 of 0.41/1.2 nM in radioisotope kinase assays, respectively.
    SK-124 displays acceptable oral bioavailability in mice, robust stability in human, rat, and mouse liver microsomes, no inhibition of cytochrome P450 enzymes.
    SK-124 exhibits no significant off-target activities at 10 µM in the Eurofins SafetyScreen44 panel, PDGFRα (IC50=15.8 nM) is the major off-target kinase.
    SK-124 engages endogenous SIK2 in murine osteocyte-like Ocy454 cells, reduces phosphorylation of SIK substrates HDAC4/HDAC5 and CRTC2 in murine Ocy454 and human Saos2 cells, promotes CRTC2 (EC50=128 nM in ) and HDAC5 nuclear translocation, and regulated SIK target gene [SOST and TNFSF11 (also known as RANKL)] expression in a PTH-like manner without causing cytotoxicity.
    Oral SK-124 (40 mg/kg) treatment increased P1NP and C terminal telopeptide (CTX) compared with oral vehicle solution in a manner similar to that of once-daily subcutaneous PTH treatmentparathyroid hormone (PTH).
    3 wk of 40 mg/kg SK-124 treatment led to changes consistent with intermittent PTH therapy and inducible SIK2/SIK3 deletion including increased trabecular bone in the primary spongiosa (PS), modest growth plate expansion, and increased TRAP-positive osteoclasts in the proximal tibia.

    Physicochemical Properties

    M.Wt 430.468
    Formula C23H22N6O3
    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-(2,6-dimethoxy-4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)phenyl)-5-ethyl-1,3,4-oxadiazole

    References

    1. Sato T, et al. Proc Natl Acad Sci U S A. 2022 Dec 13;119(50):e2214396119.

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