SGC-CBP30

Pricing Availability Delivery Time Qty
Cat.No. 4889 - SGC-CBP30 | C28H33ClN4O3
Description: Potent CBP/p300 BRD inhibitor
Chemical Name: 2-[2-(3-Chloro-4-methoxyphenyl)ethyl]-5-(dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-1,3-benzodiazole
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent CBP/p300 bromodomain (BRD) inhibitor (Kd values are 21 and 32 nM for CBP and p300 BRDs respectively). Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. 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 SGC-CBP30 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 SGC-CBP30 is reviewed on the chemical probes website.

Compound Libraries

SGC-CBP30 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 509.04
Formula C28H33ClN4O3
Storage Store at +4°C
Purity ≥98% (HPLC)
PubChem ID 72201027
InChI Key GEPYBHCJBORHCE-SFHVURJKSA-N
Smiles CC1=C(C(C)=NO1)C2=CC=C3C(N=C(CCC4=CC(Cl)=C(OC)C=C4)N3C[C@@H](N5CCOCC5)C)=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 100 mM in DMSO and to 100 mM in ethanol

Preparing Stock Solutions

The following data is based on the product molecular weight 509.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.96 mL 9.82 mL 19.64 mL
5 mM 0.39 mL 1.96 mL 3.93 mL
10 mM 0.2 mL 0.98 mL 1.96 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Gallenkamp et al (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem 9 438 PMID: 24497428

Hay et al (2014) Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J.Am.Chem.Soc. 136 9308 PMID: 24946055

Hammitzsch et al (2015) CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc.Natl.Acad.Sci.U.S.A. 112 10768 PMID: 26261308


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Citations for SGC-CBP30

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Literature in this Area

Cancer

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

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

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

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.

Pathways for SGC-CBP30

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