ERK-IN-2 is a ERK2 inhibitor with an IC 50 value of 1.8 nM. ERK-IN-2 might cause off-target toxicity and/or off-target activity at dose >10 μM .
The criteria of inhibitor probe: Inhibitor potency: goal is <100 nM (IC 50 ); Selectively with target family: >30-fold. We recommend ERK-IN-2 (MRK-ERKi) to be used at a concentration of 1 μM in cell-based experiments while not recommend doses >10 μM to be employed in any experiment.ERK-IN-2 (1 μM) has effects on cell proliferation in cancer cell lines. The IC 50 values are 214 nM; 305 nM; 91 nM and 201 nM for A375SM cell, SK-MEL 30 cell; Colo 205 cell and Lovo cell, respectively .
ERK-IN-2 (1 mpk; orally administation/0.5 mpk; intravenous injection) exhibits a DMPK value: h/r/d LM CLint: <17/235/<75 (mL/min/kg); uCLp:217 mL/min/kg; uVd 5.7 L/kg; t 1/2 : 0.4 h; rat F:13% in SD rat .