PFI-4

Alias: PFI 4; PFI4; PFI-4.
Cat No.:V0416 Purity: ≥98%
PFI-4 is a novel, potent,cell permeableand selective inhibitor of bromodomain and PHD finger-containing protein 1 (BRPF1) with antineoplastic activity.
PFI-4 Chemical Structure CAS No.: 900305-37-5
Product category: Epigenetic Reader Domain
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PFI-4 is a novel, potent, cell permeable and selective inhibitor of bromodomain and PHD finger-containing protein 1 (BRPF1) with antineoplastic activity. It inhibits BRPF1 with an IC50 of 80 nM. PFI-4 aacts by specifically binding 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. BRPF1 exists in 2 different isoforms: BRPF1A and BRPF1B. A residue insertion in the ZA loop of BRPF1A prevents binding to acetylated histone peptides. BRPF1A may act as dominant negative isoform of BRPF1 generated by alternative splicing.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
PFI-4 (1.25 µM; 7 or 11 days) suppresses development of human osteoclasts[1].
ln Vivo

Cell Assay
Cell Viability Assay[1]
Cell Types: Osteoclasts
Tested Concentrations: 1.25 µM
Incubation Duration: 7 or 11 days
Experimental Results: Dramatically reduces MMP9 secretion in osteoclasts .
Animal Protocol


References
[1]. Meier JC, et al. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630.
[2]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H24N4O3
Molecular Weight
380.44
CAS #
900305-37-5
SMILES
O=C1N(C([H])([H])[H])C2C([H])=C(C(=C([H])C=2N1C([H])([H])[H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])N([H])C(C1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])[H])=O
InChi Key
QCIJLRJBZDBVDB-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)
Chemical Name
N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Synonyms
PFI 4; PFI4; PFI-4.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 17 mg/mL (44.7 mM)
Water:<1 mg/mL
Ethanol:5 mg/mL (13.1 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6285 mL 13.1427 mL 26.2854 mL
5 mM 0.5257 mL 2.6285 mL 5.2571 mL
10 mM 0.2629 mL 1.3143 mL 2.6285 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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