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Submit ReviewSGC-CBP30
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)
Biological Activity for SGC-CBP30
SGC-CBP30 is a 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 for SGC-CBP30
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.
Technical Data for SGC-CBP30
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SGC-CBP30
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 | ||
| ethanol | 100 |
Preparing Stock Solutions for SGC-CBP30
The following data is based on the product molecular weight 509.04. 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 | 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 for SGC-CBP30
References for SGC-CBP30
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
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
If you know of a relevant reference for SGC-CBP30, please let us know.
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1 Citation for SGC-CBP30
Citations are publications that use Tocris products. Selected citations for SGC-CBP30 include:
Koh et al (2018) A conserved enhancer regulates Il9 expression in multiple lineages. Nat Commun 9 4803 PMID: 30442929
Do you know of a great paper that uses SGC-CBP30 from Tocris? Please let us know.
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