6RK73 is a potent, specific and covalent UCHL1 inhibitor with IC50 of 0.23 uM.
6RK73 displays a high selectivity over other DUBs including its closest family members UCHL3 and UCHL5.
6RK73 shows more potent inhibition than LDN57444 on UCHL1 activity in MDA-MB-436 cells by TAMRA ABP assay.
6RK73 is comparable to genetic knockdown of UCHL1.
6RK73 displays strong inhibition of the TGFβ-induced pSMAD2 and pSMAD3, and a decrease of TβRI and total SMAD protein levels in MDA-MB-436 cells, which is stronger than the effect of shRNA-mediated UCHL1 knockdown.
6RK73 potently inhibits breast cancer migration and extravasation.
