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MRT 199665

Chemical Structure : MRT 199665

CAS No.: 1456858-57-3

MRT 199665 (MRT199665)

Catalog No.: PC-61765Not For Human Use, Lab Use Only.

MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively.

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

    Biological Activity

    MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively.
    MRT 199665 also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM).
    MRT 199665 elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.

    Physicochemical Properties

    M.Wt 373.43
    Formula C18H19N3O4S
    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

    7-[(1S)-4-Hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-(methylsulfonyl)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

    References

    1. Clark K, et al. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.

    2. Darling NJ, et al. Biochem J. 2017 Feb 15;474(4):521-537.

    3. Huang HT, et al. Elife. 2017 Sep 19;6. pii: e26693.

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