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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. SGC-CBP30 can be used in protocols for the chemical reprogramming of somatic cells to iPSCs.
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.
Compound Libraries for SGC-CBP30
SGC-CBP30 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for SGC-CBP30
| M. Wt | 509.04 |
| Formula | C28H33ClN4O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1613695-14-9 |
| 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
Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 605 325 PMID: 35418683
If you know of a relevant reference for SGC-CBP30, please let us know.
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Keywords: SGC-CBP30, SGC-CBP30 supplier, SGCCBP30, CREBBP, CBP, EP300, p300, bromodomains, inhibitors, inhibits, chemical, probes, epigenetics, SGC, potent, selective, active, in, cells, permeable, structural, genomics, consortium, induced, pluripotent, stem, reprogramming, iPSC, Bromodomains, Histone, Acetyltransferases, Stem, Cell, Reprogramming, 4889, Tocris Bioscience
4 Citations for SGC-CBP30
Citations are publications that use Tocris products. Selected citations for SGC-CBP30 include:
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Koh et al (2018) A conserved enhancer regulates Il9 expression in multiple lineages. Nat Commun 9 4803 PMID: 30442929
Walter et al (2021) A Chemo-Genomic Approach Identifies Diverse Epigenetic Therapeutic Vulnerabilities in MYCN-Amplified Neuroblastoma. Front Cell Dev Biol 9 612518 PMID: 33968920
Laurent et al (2021) Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects. Cancers (Basel) 13 PMID: 34439123
Do you know of a great paper that uses SGC-CBP30 from Tocris? Please let us know.
Reviews for SGC-CBP30
Average Rating: 5 (Based on 1 Review.)
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p300 inhibition.
By
Anonymous on 10/31/2022
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: 293T
Used to inhibit p300 and downstream genes. We treated 293 cells with CBP30 and then detected p300 staining with IF. Figure: Green channel is p300 in nucleus
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