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.
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.
