TP-238 is a BPTF inhibitor. TP-238 has on target biochemical activity of 10-30 nM with CECR2 and 100-350 nM with BPTF. Negative control TP-422 is completely inactive against BPTF and CECR2. The closest off-target bromodomain inhibition is BRD9 with IC50 of 1.4 µM. TP-238 has been profiled against the panel of 338 kinases and showed no activity at 1 μM. TP-238 and TP-422 can be used at no more than 2 µM concentration in cells. Cell-based NanoBRETTM experiments measured the target engagement with both BPTF and CECR2 with EC50 in the 200-300 nM range. TP-238 shows an IC50 of 30nM against CECR2 and 350nM against BPTF in an alphascreen assay. ITC shows TP-238 with a KD of 10nM for CECR2 and 120nM for BPTF.
MedKoo Cat#: 565144
Name: TP-238
CAS#: 2415263-04-4 (free base)
Chemical Formula: C22H30N6O3S
Exact Mass: 458.2100
Molecular Weight: 458.58
Elemental Analysis: C, 57.62; H, 6.59; N, 18.33; O, 10.47; S, 6.99
The following data is based on the product molecular weight 458.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
