IC50: 0.10 µM (BCL6-corepressor interaction)[1]
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay[1].
TP-021 (BCL6-IN-8c, Compound 8c) also exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC50 = 0.72 µM). TP-021 (BCL6-IN-8c) does not exhibit significant cytotoxicity even at 30 µM[1].
The pharmacokinetic profile of TP-021 (BCL6-IN-8c, Compound 8c) is evaluated by a mouse cassette-dosing study (0.1 mg/kg iv; 1 mg/kg po). TP-021 (BCL6-IN-8c) exhibits a good pharmacokinetic profile (Cmax = 233 ng/mL, Tmax = 2 hours, MRT = 3.3 h, AUC = 1.27 mg•h/mL, F (oral bioavailability) = 79.9%)[1].