PF-CBP1 hydrochloride

SKU: orb1304414

Description

PF-CBP1 hydrochloride is a potent and selective bromodomain inhibitor of CREBBP and its paralog p300, with IC50 values of 125 nM and 363 nM, respectively. This small molecule is a valuable chemical probe for epigenetic research, used in vitro and in vivo to study the roles of these acetyl-lysine reader proteins in transcription, cell signaling, and disease models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2070014-93-4
• MW: 525.08
• Purity: 99.02% (May vary between batches)
• Formula: C₂₉H₃₇ClN₄O₃
• SMILES: Cl.CCCOc1ccc(CCc2nc3cc(ccc3n2CCN2CCOCC2)-c2c(C)noc2C)cc1
• Target: Epigenetic Reader Domain,Histone Acetyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.81 mM);DMSO:45 mg/mL (85.7 mM)

Bioactivity

• Target IC50:
  BRD4:20 μM (Kd)|p300/CBP:363nM|CREBBP:125nM
• 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.

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

CREBBP, cortical, HistoneAcetyltransferase, Histone Acetyltransferase, HATs, HAT, Inhibitor, epilepsy, EpigeneticReaderDomain, Epigenetic Reader Domain, inhibit, inflammatory, p300/CBP, parkinson's disease, neuron, neurological disorder, RGS4, PF CBP1 hydrochloride, PF-CBP1, PF-CBP1 HCl, PFCBP1 hydrochloride, PF-CBP1 Hydrochloride, PF-CBP-1 hydrochloride

Compound Identifiers

PubChem CID

119081416