CPI-644
CAS No. : 1904647-34-2
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| Cat. No. : | HY-122081 |
| M.Wt: | 357.43 |
| Formula: | C18H19N3O3S |
| Purity: | >98 % |
| Solubility: |
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[1].
In Vitro: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].
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