usp1-uaf1

ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively.

I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.

SJB2-043, an inhibitor of USP1-UAF1, has an IC50 of 544 nM.

C527 is a potent pan DUB enzyme inhibitor with a high affinity for the USP1/UAF1 complex (IC50=0.88 μM).

USP1-IN-3 is a selective inhibitor of USP1, effectively inhibiting USP1-UAF1 with an IC50 of less than 30 nM. USP1-IN-3 is utilized for cancer research.

USP1-IN-7 (Compound 3), a potent inhibitor of ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, exhibits an inhibition concentration (IC 50) of ≤50 nM. It also effectively inhibits the proliferation of MDA-MB-436 cells at similar concentrations [1].