CPI-637

Name: CPI-637
Brand: TargetMol
SKU: T6811
Price: 283 CNY
Availability: InStock
Rating: 5 (10 reviews)

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产品编号 T6811Cas号 1884712-47-3

别名 CPI 637

CPI-637 是一种选择性和细胞活性的苯二氮卓 CBP/EP300 溴结构域抑制剂，其对 CBP、EP300和 BRD4 BD-1的 IC50值分别为 0.03、0.051 和 11.0 μM，对 CBP 的 EC50值为 0.3 μM。

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产品编号 T6811 别名 CPI 637Cas号 1884712-47-3

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产品介绍

生物活性

产品描述	CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
靶点活性	BRD4 BD1:11 μM, CBP:0.03 μM, EP300:0.051 μM
体外活性	CPI-637 inhibits MYC expression in AMO-1 cells (EC50=0.60 μM)[1].
激酶实验	Ki Determination: Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis.
细胞实验	AMO-1 cells (DSMZ) were plated at 20,000 cells/well in 96-well plates in Iscove's Modified Dulbecco's Medium supplemented with 10% fetal calf serum. Cells were treated for 6 h with a dose titration of CPI-637 starting from a 5 μM top concentration. After 6 h, cells were lysed and processed for QuantiGene Plex expression analysis and data were collected on a MAGPIX multiplex Luminex instrument.(Only for Reference)
别名	CPI 637

化学信息

分子量	386.45
分子式	C₂₂H₂₂N₆O
CAS No.	1884712-47-3
Smiles	C[C@@H]1CC(=O)Nc2cccc(-c3ccc4n(C)nc(-c5cnn(C)c5)c4c3)c2N1
密度	1.38 g/cm3 (Predicted)