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TP-238 hydrochloride is a highly potent and selective dual CECR2/BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases.


| Description | TP-238 hydrochloride is a highly potent and selective dual CECR2/BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases. |
| Targets&IC50 | BRD9:5.9 (pIC50), CECR2:30 nM, CECR2:7.5 (pIC50), CECR2:10 nM (Kd), BPTF:6.5 (pIC50), BPTF:120 nM (Kd), BPTF:350 nM |
| In vitro | TP-238 exhibits specificity and potency towards CECR2 and BPTF, with an on-target biochemical activity measured at 10-30 nM for CECR2 and 100-350 nM for BPTF. In an Alpha screen assay, TP-238 demonstrates effectiveness, evidencing a pIC50 of 7.5 for CECR2 and 6.5 for BPTF. Further analysis using Isothermal Titration Calorimetry (ITC) reveals TP-238 binds with a dissociation constant (Kd) of 10 nM for CECR2 and 120 nM for BPTF[1][2]. |
| Molecular Weight | 495.04 |
| Formula | C22H31ClN6O3S |
| Cas No. | 2415263-05-5 |
| Smiles | Cl.CN(C)CCCOc1ccc(cc1)-c1cc(NCCCn2cccn2)nc(n1)S(C)(=O)=O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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