For research use only. Not for therapeutic Use.
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].
TP-238 has on target biochemical activity of 10-30 nM with CECR2 and 100-350 nM with BPTF. TP-238 displays potency for both CECR2 (pIC50 of 7.5) and BPTF (pIC50 of 6.5) in an Alpha screen assay. Isothermal titration calorimetry (ITC) shows TP-238 with a Kd of 10 nM for CECR2 and 120 nM for BPTF[1][2].
| Catalog Number | I037426 |
| CAS Number | 2415263-05-5 |
| Synonyms | 6-[4-[3-(dimethylamino)propoxy]phenyl]-2-methylsulfonyl-N-(3-pyrazol-1-ylpropyl)pyrimidin-4-amine;hydrochloride |
| Molecular Formula | C22H31ClN6O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C22H30N6O3S.ClH/c1-27(2)13-6-16-31-19-9-7-18(8-10-19)20-17-21(26-22(25-20)32(3,29)30)23-11-4-14-28-15-5-12-24-28;/h5,7-10,12,15,17H,4,6,11,13-14,16H2,1-3H3,(H,23,25,26);1H |
| InChIKey | FHVADRKEPFRFFF-UHFFFAOYSA-N |
| SMILES | CN(C)CCCOC1=CC=C(C=C1)C2=CC(=NC(=N2)S(=O)(=O)C)NCCCN3C=CC=N3.Cl |
| Reference | [1]. Michael A Clegg, et al. Advancements in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem. 2019 Feb 19;14(4):362-385. [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. |
