PF-CBP1

SKU: orb1303491

Description

PF-CBP1 HCl is a potent and selective bromodomain inhibitor targeting CREBBP (IC50 = 125 nM) and its paralog p300 (IC50 = 363 nM). This small molecule is a valuable chemical probe for epigenetic research, enabling the study of BET-independent transcriptional regulation in both cellular and in vivo models of cancer and other diseases.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1962928-21-7
• MW: 488.62
• Purity: 99.91%
• Formula: C₂₉H₃₆N₄O₃
• SMILES: C(CN1CCOCC1)N2C=3C(N=C2CCC4=CC=C(OCCC)C=C4)=CC(=CC3)C=5C(C)=NOC5C
• Target: Epigenetic Reader Domain
• Solubility: DMSO:50 mg/mL (102.33 mM)

Bioactivity

• Target IC50:
  CREBBP:125 nM|p300 BD:363 nM
• In Vitro:
  PF-CBP1 modulates key inflammatory genes in primary macrophages, downregulates RGS4 in neurons (a target linked to Parkinson's disease), and exhibits 139-fold selectivity over BRD4 in biochemical assays and >105-fold selectivity by ITC. PF-CBP1 is a potent EP300 inhibitor with no cytotoxicity in macrophages and no hepatotoxicity in cell-based models at non-toxic concentrations.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Epigenetic Reader Domain, EpigeneticReaderDomain, Inhibitor, CREB, PF-CBP-1, PF-CBP1, PFCBP1, PF CBP1

Compound Identifiers

PubChem CID

119081417