Biochem/physiol Actions
SJB2-043 is a ubiquitin-specific protease USP1 inhibitor (IC50 = 544 nM using USP1/UAF1 complex) that exhibits anti-proliferation efficacy against chronic and acute myeloid leukemia lines (IC50 <2 µM; K562, OCI-AML3, SK-NO1, U937) and primary acute myelogenous leukemia (AML) patient-derived leukemic cells by promoting the degradation of transcription factor DNA binding 1 (ID1). SJB2-043 is also reported to be an allosteric site-targeting inhibitor against PLPro (IC50 = 0.56 μM), the papain-like cysteine protease with deubiquitination and deISGylation activities that suppress host innate immune responses toward SARS-CoV-2 infection.
Ubiquitin-specific protease USP1 inhibitor with anti-leukemia efficacy. Also reported to inhibit SARS-CoV-2 papain-like cysteine protease PLPro.