PFI 4Potent and selective BRPF1 Bromodomain inhibitor CAS# 900305-37-5 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 900305-37-5 | SDF | Download SDF |
| PubChem ID | 40642506 | Appearance | Powder |
| Formula | C21H24N4O3 | M.Wt | 380.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 26 mg/mL (68.34 mM; Need ultrasonic and warming) | ||
| Chemical Name | N-(1,3-dimethyl-2-oxo-6-pyrrolidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide | ||
| SMILES | CN1C2=CC(=C(C=C2N(C1=O)C)N3CCCC3)NC(=O)C4=CC=CC=C4OC | ||
| Standard InChIKey | QCIJLRJBZDBVDB-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. Disrupts BRPF1 binding to histone H3.3. Cell permeable. |
PFI 4 Dilution Calculator
PFI 4 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6285 mL | 13.1427 mL | 26.2854 mL | 52.5707 mL | 65.7134 mL |
| 5 mM | 0.5257 mL | 2.6285 mL | 5.2571 mL | 10.5141 mL | 13.1427 mL |
| 10 mM | 0.2629 mL | 1.3143 mL | 2.6285 mL | 5.2571 mL | 6.5713 mL |
| 50 mM | 0.0526 mL | 0.2629 mL | 0.5257 mL | 1.0514 mL | 1.3143 mL |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2629 mL | 0.5257 mL | 0.6571 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PFI 4 is a cell permeable, potent and selective inhibitor of BRPF1 Bromodomain with pIC50 and pKd values of 7.1 and 8.0 [1].
The BRPF (bromodomain and PHD finger-containing) family BRPF1, BRPF2/BRD1, and BRPF3 operate as scaffolds to assemble MYST-family histone acetyltransferases (HATs) complexes. BRPF1 is a component of complexes containing the MOZ/MORF transcriptional coactivators and links the catalytic HATs to the other subunits ING5 and hEAF6.8. BRPF1 is important for maintaining skeletal development and Hox gene expression in fish [1].
In the BROMOscan panel of 35 bromodomain binding assays, PFI 4 exhibited excellent BRPF1 potency with pKd value of 8.0 and excellent selectivity over other bromodomains. In a cellular protein interaction assay, PFI 4 displaced NanoLuc-tagged BRPF1 bromodomain from Halotagged
histone H3.3 and disrupted chromatin binding [1].
Reference:
[1]. Demont EH, Bamborough P, Chung CW, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett, 2014, 5(11): 1190-1195.
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The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.[Pubmed:26139243]
Cancer Res. 2015 Sep 15;75(18):3865-3878.
The SWI/SNF multisubunit complex modulates chromatin structure through the activity of two mutually exclusive catalytic subunits, SMARCA2 and SMARCA4, which both contain a bromodomain and an ATPase domain. Using RNAi, cancer-specific vulnerabilities have been identified in SWI/SNF-mutant tumors, including SMARCA4-deficient lung cancer; however, the contribution of conserved, druggable protein domains to this anticancer phenotype is unknown. Here, we functionally deconstruct the SMARCA2/4 paralog dependence of cancer cells using bioinformatics, genetic, and pharmacologic tools. We evaluate a selective SMARCA2/4 bromodomain inhibitor (PFI-3) and characterize its activity in chromatin-binding and cell-functional assays focusing on cells with altered SWI/SNF complex (e.g., lung, synovial sarcoma, leukemia, and rhabdoid tumors). We demonstrate that PFI-3 is a potent, cell-permeable probe capable of displacing ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromatin, yet contrary to target knockdown, the inhibitor fails to display an antiproliferative phenotype. Mechanistically, the lack of pharmacologic efficacy is reconciled by the failure of bromodomain inhibition to displace endogenous, full-length SMARCA2 from chromatin as determined by in situ cell extraction, chromatin immunoprecipitation, and target gene expression studies. Furthermore, using inducible RNAi and cDNA complementation (bromodomain- and ATPase-dead constructs), we unequivocally identify the ATPase domain, and not the bromodomain of SMARCA2, as the relevant therapeutic target with the catalytic activity suppressing defined transcriptional programs. Taken together, our complementary genetic and pharmacologic studies exemplify a general strategy for multidomain protein drug-target validation and in case of SMARCA2/4 highlight the potential for drugging the more challenging helicase/ATPase domain to deliver on the promise of synthetic-lethality therapy.
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.[Pubmed:25408830]
ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.
