PF-CBP1 HCl

Catalog No.S8180 Batch:S818001

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Technical Data

Formula

C29H36N4O3.HCl
Molecular Weight 525.08 CAS No. 2070014-93-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (190.44 mM)
Ethanol 100 mg/mL (190.44 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.)

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Biological Activity

Description PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
Targets
CREBBP [1]
(Cell-free assay)		 p300/CBP [1]
(Cell-free assay)
125nM 363nM
In vitro PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 down regulates RGS4 in neurons, a target linked to Parkinson's disease.It is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC.PF-CBP1 is also a potent inhibitor of EP300 and possesses no cytotoxicity in macrophages, and hepatotoxicity in cell-based models as long as the concentration is not very high[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    mouse J774 macrophage-like cell line

  • Concentrations

    0.1-10 μM

  • Incubation Time

    30min

  • Method

    Cells are pretreated with the probes PF-CBP1, ISOX-INACT, or ISOX-DUAL starting at 10 μM concentrations, and then serially diluted to 0.1 μM. After 30 min, the cells are treated with LPS to induce gene transcription and the expression levels of interleukin-6 (IL-6), IL-1β, and interferon-β (IFN-β)(which are known to be induced after 4 h of LPS exposure) are analyzed by RT-PCR. Probe PF-CBP1 moderately reduces LPS-induced IL-6 and IFN-β expression at 10 μM, and a decrease in IL-1β expression is evident at 3 μM. 

Selleck's PF-CBP1 HCl has been cited by 5 publications

Brain milieu induces early microglial maturation through the BAX-Notch axis [ Nat Commun, 2022, 13-1:6117] PubMed: 36253375
The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress [ Nat Aging, 2021, 1(2):165-178] PubMed: 33718883
Interferon-γ Signaling in Melanocytes and Melanoma Cells Regulates Expression of CTLA-4 [ Cancer Res, 2018, 78(2):436-450] PubMed: 29150430
Interferon-γ Signaling in Melanocytes and Melanoma Cells Regulates Expression of CTLA-4 [ Cancer Res, 2018, 78(2):436-450] PubMed: 29150430
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193

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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.