product name PFI-4
Description: PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. PFI-4 specifically binds to BRPF1B with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 of 250nM, while showing no effect on BRPF1A. BRPF1A may act as dominant negative isoform of BRPF1 generated by alternative splicing.
References: ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
380.44
Formula
C21H24N4O3
CAS No.
900305-37-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 17 mg/mL (44.7 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (13.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19419525
| In Vitro |
In vitro activity: PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3. Kinase Assay: Cell Assay: Disrupts BRPF1 binding to histone H3.3. PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP, inhibiting binding to tri-acetylated histone 4 (residues 1-21). It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 μM) and is selective for BRPF1 over BRPF2 and BRPF3. PFI-4 is potent in cells, with an IC50 value of 250 nM. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5 |
