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首页-小分子抑制剂&激动剂-Autophagy-Salt Inducible Kinase (SIK)-MRT199665
MRT199665

Chemical Structure : MRT199665

CAS No.: 1456858-57-3

MRT199665 (MRT 199665, MRT-199665)

货号: PC-61765Not For Human Use, Lab Use Only.

MRT199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    MRT199665 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.

    物理化学性质&存储条件

    分子量 373.43
    分子式 C18H19N3O4S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

    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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