TABLE 1.
Summary of biochemical and cell assay results
ML364 | Compound 2 | |
---|---|---|
USP2 Di-Ub IQF Lys-48-l4 (IC50) | 1.1 μm | Inactive |
USP2 Di-Ub IQF Lys-63-3 (IC50) | 1.7 μm | Inactive |
HCT116 cell viability (EC50) | 3 μm | Inactive |
Mino cell viability (EC50) | 4.7 μm | Inactive |
HCT116 Clonogenic (EC50) | 3.6 μm | Inactive |
HCT116 Acumen cell cycle (EC50) | 2 μm | Inactive |
HCT116 flow, cell cycle | Arrest in G1 | Inactive |
Mino flow, cell cycle | Arrest in G1 | Inactive |
Western HCT116, cyclin D1 destabilization | 0.97 μm | Inactive |
Western Mino, cyclin D1 destabilization | 8.5 μm | Inactive |
Caspase 6 (IC50) | Inactive | Inactive |
Caspase 7 (IC50) | Inactive | Inactive |
USP8 Di-Ub IQF Lys-48-2 (IC50) | 0.95 μm | Inactive |
USP20 Di-Ub IQF Lys-48-2 (IC50) | Inactive | Inactive |
MMP1 (IC50) | Inactive | NDa |
MMP9 (IC50) | Inactive | ND |
102 kinases screened at 10 μm | Inactive | ND |
a ND means not determined.