TP-238
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.
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- No. CAS: 2415263-04-4
- Fòrmula: C22H30N6O3S
- Peso molecular:458.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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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) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2415263-04-4
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Peso molecular 458.58
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Fòrmula C22H30N6O3S
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SMILES
CN(C)CCCOC1=CC=C(C=C1)C2=CC(NCCCN3N=CC=C3)=NC(S(=O)(C)=O)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Michael A Clegg, et al. Advancements in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem. 2019 Feb 19;14(4):362-385. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TP-238 Related Classifications
HY-114205 Related Classifications
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