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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1904647-34-2
- 分子式: C18H19N3O3S
- 分子量:357.43
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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. Further protocols information, click here.
化学情報
-
CAS 番号 1904647-34-2
-
分子量 357.43
-
分子式 C18H19N3O3S
-
SMILES
C(=C/C1=C(S(N)(=O)=O)C=CC=C1)\C2=C3C(NC(=O)C[C@@H](C)N3)=CC=C2
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)