2415263-05-5

TP-238 HCl is a chemical probe for the bromodomains of cat eye syndrome chromosome region, candidate 2 (CECR2) and bromodomain PHD finger transcription factor (BPTF). TP-238 binds to CECR2 and BPTF with KD values of 10 and 120 nM, respectively, in an isothermal titration calorimetry (ITC) assay and IC50 values of 30 and 350 nM, respectively, in an AlphaScreen? assay.

TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases[1][2].

CECR2: 30 nM (IC₅₀); CECR2: 10 nM (Kd); CECR2: 7.5 (pIC₅₀); BPTF: 350 nM (IC₅₀); BPTF: 120 nM (Kd); BPTF: 6.5 (pIC₅₀); BRD9: 5.9 (pIC₅₀)

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[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