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UBE2T/FANCL inhibitor UC2

Chemical Structure : UBE2T/FANCL inhibitor UC2

CAS No.: 1359415-02-3

UBE2T/FANCL inhibitor UC2 (UC2)

Catalog No.: PC-73071Not For Human Use, Lab Use Only.

UBE2T/FANCL inhibitor UC2 (UC2) is a specific small-molecule inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation, inhibits the ubiquitylation of GST-FANCL RINGwith IC50 of 14.8 uM in HTRF ubiquitylation assay.

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    Biological Activity

    UBE2T/FANCL inhibitor UC2 (UC2) is a specific small-molecule inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation, inhibits the ubiquitylation of GST-FANCL RINGwith IC50 of 14.8 uM in HTRF ubiquitylation assay.
    UC2 did not affect ubiquitylation of either UBE2T or UBE1, exhibited some degree of selectivity for FANCL-dependent ubiquitylation.
    UC2 completely inhibited the ubiquitylation of GST-FANCLRING at 100 uM.
    UC2 demonstrated activity against the Fanconi anemia (FA) pathway in cells.
    UC2 sensitizes cells to the DNA cross-linking agent, carboplatin.
    The Fanconi anemia (FA) pathway, also known as the FA/BRCA pathway, is required for the repair of DNA interstrand cross-links (ICLs).
    Key components of the FA pathway are the ubiquitin E2 enzyme, UBE2T (FANCT) and the RING-type ubiquitin E3 ligase, FANCL.

    Physicochemical Properties

    M.Wt 357.506
    Formula C19H31N7
    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

    5-(4-ethylpiperazin-1-yl)-7-methyl-2-((2-methylpiperidin-1-yl)methyl)-[1,2,4]triazolo[1,5-a]pyridine

    References

    1. Cornwell MJ, et al. ACS Chem Biol. 2019 Oct 18;14(10):2148-2154.

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