Cell penetrant, potent and selective chemical probe for the ubiquitin binding domain (UBD) of HDAC6 (histone deacetylase 6)
SGC-UBD253 is a cell penetrant, potent and selective chemical probe for the ubiquitin binding domain (UBD) of HDAC6 (histone deacetylase 6). SGC-UBD253 potently binds to HDAC6 UBD (KD = 84 nM) and inhibits the HDAC6-ISG15 interaction (EC50 = 1.9 µM).
Journal of medicinal chemistry, 61(10), 4517-4527 (2018-05-10)
HDAC6 plays a central role in the recruitment of protein aggregates for lysosomal degradation and is a promising target for combination therapy with proteasome inhibitors in multiple myeloma. Pharmacologically displacing ubiquitin from the zinc-finger ubiquitin-binding domain (ZnF-UBD) of HDAC6 is
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