CPI-644
CPI-644 is a selective EP300/CBP bromodomain inhibitor, with an IC50 of 0.18 µM against the CBP bromodomain. CPI-644 reduces the proportion of FOXP3+ cells and downregulates the expression of LAG-3, CTLA-4 and PD-1. CPI-644 can be used in cancer-related research.
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- CAS. Nr.: 1904647-34-2
- Formel: C18H19N3O3S
- Molecular Weight:357.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
CPI-644 potently and selectively inhibits the purified CBP bromodomain in AlphaLISA peptide competition assays, with an IC50 of 0.18 μM[1].
CPI-644 binds tightly to the purified CBP bromodomain, with a Kd value of 0.084 μM measured by ITC[1].
CPI-644 inhibits the cellular interaction between the bromodomains of CBP and EP300 and histone H3.3 in HEK293 cells, with EC50 values of 0.53 μM and 0.36 μM, respectively[1].
CPI-644 potently inhibits the differentiation of naive human CD4+CD45RA+ T cells into FOXP3+ Treg, with an IC50 of 1.8 μM[1].
CPI-644 dose-dependently reduces the expression of Treg inhibitory markers LAG-3, CTLA-4 and PD-1 in in vitro differentiated regulatory T cells (Treg), with EC50 values of 0.9 μM, 1.8 μM and 4.3 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1904647-34-2
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Molecular Weight 357.43
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Formel C18H19N3O3S
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SMILES
C(=C/C1=C(S(N)(=O)=O)C=CC=C1)\C2=C3C(NC(=O)C[C@@H](C)N3)=CC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)