Menu

TP-021

2D structure
Target BCL6 
Targeted domain Bric-a-brac (BTB) domain
Mode of action Inhibitor
Control TP-021n
Orthogonal probe CCT369260  BI-3802  BI-3812 
Recommended cellular usage concentration 1 -10 µM
In vivo use yes
Synonyms BCL6 inhibitor 8c, BCL6-IN-8c
Donated by Takeda


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: BCL6: IC50 = 100 nM (ELISA)
Selectivity within target family: > 30-fold Compound is PPI (Protein Protein Inhibition) inhibitor targetting non-conserved sites
Selectivity outside target family TP-021 and TP-021n show no significant inhibition at 1 μM in Takeda in house kinase panel (344 targets); Clean PDSP scan
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: IC50 = 0.72 μM cell-based mammalian two-hybrid assay (M2H)
Control compound (100 times less potent than the probe) Surpasses criterion: IC50 = 110 μM (ELISA), more than 1,000-fold weaker than the probe candidate; Clean PDSP scan