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.
For research use only. We do not sell to patients.
- CAS No.: 2415263-04-4
- Formula: C22H30N6O3S
- Molecular Weight:458.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All SWI/SNF Complex Isoforms
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Biological Activity
Description
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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) |
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[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2415263-04-4
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Molecular Weight 458.58
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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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