TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC 50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC 50 of 5.9 and is less active against other 338 kinases.
性状
Solid
IC50 & Target[1][2]
CECR2 30 nM (IC50) CECR2 10 nM (Kd)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (202.00 mM; Need ultrasonic)配制储备液