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Submit ReviewI-CBP 112
Description: Selective CBP/p300 BRD inhibitor
Chemical Name: 1-[7-(3,4-Dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-2,3,4,5-tetrahydro-1,4-benzoxazepin-4-yl]propan-1-one
Purity: ≥98% (HPLC)
Biological Activity
CBP/p300 bromodomain inhibitor (IC50 values are 0.142-0.17 and 0.625 μM for CBP and p300 respectively). Selective for CBP and p300 over ATAD2, BAZ2B, BRD2(2), BRD4(1), PB1(5), PCAF, PHIP(2) and TIF1α bromodomains in a BLI assay. Accelerates FRAP recovery in cells at a concentration of 1 μM.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the I-CBP 112 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of I-CBP 112 is reviewed on the chemical probes website.
Compound Libraries
I-CBP 112 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 468.59 |
| Formula | C27H36N2O5 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1640282-31-0 |
| PubChem ID | 90488984 |
| InChI Key | YKNAKDFZAWQEEO-IBGZPJMESA-N |
| Smiles | COC(C(OC)=C1)=CC=C1C2=CC(OC[C@H]3CCCN(C)C3)=C(OCCN(C(CC)=O)C4)C4=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 | ||
| 1eq. HCl | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 468.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.67 mL | 21.34 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Gallenkamp et al (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem 9 438 PMID: 24497428
If you know of a relevant reference for I-CBP 112, please let us know.
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Keywords: I-CBP 112, I-CBP 112 supplier, I-CBP112, CREBBP, EP300, bromodomains, selective, inhibitors, inhibits, chemical, probes, SGC, epigenetics, structural, genomics, consortium, Bromodomains, Histone, Acetyltransferases, 4891, Tocris Bioscience
Citations for I-CBP 112
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- Bromodomains
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.