Size | Price | Stock | Qty |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
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.
ln Vitro |
PFI-4 (1.25 µM; 7 or 11 days) suppresses development of human osteoclasts[1].
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ln Vivo |
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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 . |
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Animal Protocol |
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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. |
Molecular Formula |
C21H24N4O3
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Molecular Weight |
380.44
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CAS # |
900305-37-5
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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
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InChi Key |
QCIJLRJBZDBVDB-UHFFFAOYSA-N
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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)
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Chemical Name |
N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
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.
(2) Be sure to add the solvent(s) in order.