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首页-小分子抑制剂&激动剂-Tyrosine Kinase-DYRK-CaNDY
CaNDY

Chemical Structure : CaNDY

CAS No.: 1549853-04-4

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CaNDY (CLK inhibitor CaNDY)

货号: PC-72581Not For Human Use, Lab Use Only.

CaNDY is a highly potent rectifier of the aberrant splicing, potently inhibits DYRK1A, DYRK1B, CLK1/CLK2 with IC50 of 21.6/68.3/116 nM in in vitro kinase assays.

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

    生物&药学活性

    CaNDY is a highly potent rectifier of the aberrant splicing, potently inhibits DYRK1A, DYRK1B, CLK1/CLK2 with IC50 of 21.6/68.3/116 nM in in vitro kinase assays.
    CaNDY is a potent and selective inhibitor of DYRK family kinases, CaNDY induces selective degradation of DYRK1A, and inhibits catalytic activity of recombinant DYRK1A with IC50 value of 7.9 nM by competing with ATP, antagonizes the CDC37 interaction with DYRK1A.
    CaNDY demonstrated CFTR pseudo exon suppression with EC50 of 1.2 uM, 20.4 times lower than that of TG003.
    Splice modulation by CaNDY is mediated by its CLK-inhibition activity.
    CaNDY, but not CFTR modulator VX-809, rescues mature CFTR expression from the CFTR gene with the 3,849 + 10 kb C>T mutation, suppresses SRSF phosphorylation.
    CaNDY (3 uM) treatment rescued CFTR channel activity from CFTRC>T-GFP at an extent comparable to that of CFTRWT-GFP, demonstrating a restoration of functional CFTR expression.

    物理化学性质&存储条件

    分子量 248.3
    分子式 C12H12N2O2S
    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

    5-((2,3-dihydrobenzofuran-5-yl)methyl)-2-iminothiazolidin-4-one

    参考文献

    1. Saiko Shibata, et al. Cell Chem Biol. 2020 Dec 17;27(12):1472-1482.e6.

    2. Rie Sonamoto, et al. Sci Rep. 2015 Aug 3;5:12728.

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