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SGC-CBP30

Catalog #: 4889
4 Citations Datasheet
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SGC-CBP30 | CAS No. 1613695-14-9 | Bromodomain Inhibitors
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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%

Product Details
Citations (4)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.

Technical Data

M.Wt:
509.04
Formula:
C28H33ClN4O3
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1613695-14-9

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.

Additional Information

Licensing Caveats:
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.

Background References

  1. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.
    Hay et al.
    J.Am.Chem.Soc., 2014;136:9308
  2. Bromodomains and their pharmacological inhibitors.
    Gallenkamp et al.
    ChemMedChem, 2014;9:438
  3. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
    Hammitzsch et al.
    Proc.Natl.Acad.Sci.U.S.A., 2015;112:10768

Product Datasheets

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Citations for SGC-CBP30

The citations listed below are publications that use Tocris products. Selected citations for SGC-CBP30 include:

4 Citations: Showing 1 - 4

  1. Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL.
    Authors: Christopher J Et al.
    Cancer Res  2022;82:3375-3393
  2. A Chemo-Genomic Approach Identifies Diverse Epigenetic Therapeutic Vulnerabilities in MYCN-Amplified Neuroblastoma.
    Authors: Walter Et al.
    Front Cell Dev Biol  2021;9:612518
  3. Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects.
    Authors: Laurent Et al.
    Cancers (Basel)  2021;13
  4. A conserved enhancer regulates Il9 expression in multiple lineages.
    Authors: Koh Et al.
    Nat Commun  2018;9:4803

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