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CPI-637

Catalog No.GC10382

CBP/EP300 bromodomain inhibitor

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CPI-637 Chemical Structure

Cas No.: 1884712-47-3

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10mg
$73.00
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50mg
$265.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 0.03 and 11.0 μM for CBP/EP300 and BRD4, respectively.

CPI-637 is a CBP/EP300 bromodomain inhibitor.

It has been reported that among bromodomain-containing proteins implicated in various disease pathways, cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), which is a highly homologous pair of bromodomain-containing transcriptional coactivators, are of great interest as potential drug targets due to their reported involvement in a variety of disease states.

In vitro: Previous study found that CPI-637 was potent against EP300, and its opposite enantiomer showed a over 200-fold loss in potency. Moreover, the biochemical potency of CPI-637 translated well into cells with CBP BRET EC50 of 0.3 μM, and CPI-637 demonstrated a more than 700-fold selectivity over the BET family of bromodomains. In addition, CPI-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against BRD9. Furthermore, it was found that CPI-637 was able to inhibit the expression of MYC with an EC50 of 0.60 μM in a cellular assay,. [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, CPI-637 is still in the preclinical development stage.

Reference:
[1] Taylor, A.  M. et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).

Chemical Properties

Cas No. 1884712-47-3 SDF
Chemical Name (S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one
Canonical SMILES O=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@@H](C)C1
Formula C22H22N6O M.Wt 386.45
Solubility ≥ 19.3mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5877 mL 12.9383 mL 25.8766 mL
5 mM 0.5175 mL 2.5877 mL 5.1753 mL
10 mM 0.2588 mL 1.2938 mL 2.5877 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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