SGC-CBP30

Catalog No.S7256 Batch:S725606

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Technical Data

Formula

C28H33ClN4O3
Molecular Weight 509.04 CAS No. 1613695-14-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (196.44 mM)
Ethanol 25 mg/mL (49.11 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
Targets
CREBBP [1]
(Cell-free assay)		 EP300 [1]
(Cell-free assay)
21 nM 38 nM
In vitro

As a CREBBP/EP300-selective chemical probe, SGC-CBP30 shows moderate cytotoxicity in U2OS cells and HeLa cells. [1]
Features CREBBP/EP300-selective chemical probe.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    COLO-320-HSR cells

  • Concentrations

    20 μM

  • Incubation Time

    6 h

  • Method

    Cells were then treated for 6 hours with 20μM SGC-SCP30 or DMSO.
Animal Study:

[3]
  • Animal Models

    Sprague-Dawley rats

  • Dosages

    25 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Cell, 2018, 175(1):186-199]

Data from [Data independently produced by , , J Proteome Res, 2017, 16:1743−1752]

Data from [Data independently produced by , , Biomed Pharmacother, 2018, 106:1727-1733]

Selleck's SGC-CBP30 has been cited by 32 publications

NFYC-37 promotes tumor growth by activating the mevalonate pathway in bladder cancer [ Cell Rep, 2023, 42(8):112963] PubMed: 37561631
Chemical-induced epigenome resetting for regeneration program activation in human cells [ Cell Rep, 2023, 42(6):112547] PubMed: 37224020
Long non-coding RNA ACTA2-AS1 promotes ductular reaction by interacting with the p300/ELK1 complex [ J Hepatol, 2022, 76(4):921-933] PubMed: 34953958
Structural insights into p300 regulation and acetylation-dependent genome organisation [ Nat Commun, 2022, 13(1):7759] PubMed: 36522330
DBC1 is a key positive regulator of enhancer epigenomic writers KMT2D and p300 [ Nucleic Acids Res, 2022, gkac585] PubMed: 35801925
Acetylation of Checkpoint suppressor 1 enhances its stability and promotes the progression of triple-negative breast cancer [ Cell Death Discov, 2022, 8(1):474] PubMed: 36450706
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147] PubMed: 36371227
Transcriptional Activation of Ecdysone-Responsive Genes Requires H3K27 Acetylation at Enhancers [ Int J Mol Sci, 2022, 23(18)10791] PubMed: 36142704
ecDNA hubs drive cooperative intermolecular oncogene expression [ Nature, 2021, 10.1038/s41586-021-04116-8] PubMed: 34819668
A PGE2-MEF2A axis enables context-dependent control of inflammatory gene expression [ Immunity, 2021, S1074-7613(21)00222-3] PubMed: 34129840

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.