TP-238 hydrochloride is a highly potent and selective dual CECR2/BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases.

TP-238 exhibits specificity and potency towards CECR2 and BPTF, with an on-target biochemical activity measured at 10-30 nM for CECR2 and 100-350 nM for BPTF. In an Alpha screen assay, TP-238 demonstrates effectiveness, evidencing a pIC50 of 7.5 for CECR2 and 6.5 for BPTF. Further analysis using Isothermal Titration Calorimetry (ITC) reveals TP-238 binds with a dissociation constant (Kd) of 10 nM for CECR2 and 120 nM for BPTF[1][2].