Uses
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases[1][2].
IC 50
CECR2: 30 nM (IC
50); CECR2: 10 nM (Kd); CECR2: 7.5 (pIC
50); BPTF: 350 nM (IC
50); BPTF: 120 nM (Kd); BPTF: 6.5 (pIC
50); BRD9: 5.9 (pIC
50)
References
[1] Michael A Clegg, et al. Advancements in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem. 2019 Feb 19;14(4):362-385. DOI:
10.1002/cmdc.201800738[2] Peter D Ycas, et al. New Inhibitors for the BPTF Bromodomain Enabled by Structural Biology and Biophysical Assay Development. Org Biomol Chem. 2020 Jun 26. DOI:
10.1039/d0ob00506a