PFI-1 (PF-6405761)BET inhibitor CAS# 1403764-72-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1403764-72-6 | SDF | Download SDF |
| PubChem ID | 71271629 | Appearance | Powder |
| Formula | C16H17N3O4S | M.Wt | 347.39 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 33.33 mg/mL (95.94 mM; Need ultrasonic) | ||
| Chemical Name | 2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide | ||
| SMILES | CN1CC2=C(C=CC(=C2)NS(=O)(=O)C3=CC=CC=C3OC)NC1=O | ||
| Standard InChIKey | TXZPMHLMPKIUGK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20) | ||
| 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 BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC50 values are 98 and 220 nM respectively). Induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable. |
PFI-1 (PF-6405761) Dilution Calculator
PFI-1 (PF-6405761) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8786 mL | 14.393 mL | 28.7861 mL | 57.5722 mL | 71.9652 mL |
| 5 mM | 0.5757 mL | 2.8786 mL | 5.7572 mL | 11.5144 mL | 14.393 mL |
| 10 mM | 0.2879 mL | 1.4393 mL | 2.8786 mL | 5.7572 mL | 7.1965 mL |
| 50 mM | 0.0576 mL | 0.2879 mL | 0.5757 mL | 1.1514 mL | 1.4393 mL |
| 100 mM | 0.0288 mL | 0.1439 mL | 0.2879 mL | 0.5757 mL | 0.7197 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-1 (PF-6405761) is a selective inhibitor of BET for Brd4 and Brd2 with IC50 value of 220 nM and 98 nM, respectively [1].
BET family are transcriptional regulators which consist of Brd2, Brd3, Brd4 and BRDT and play a pivotal role in cell proliferation, cell cycle progression, and apoptosis. It has been shown that Brd4 involves in the survival of many diverse tumors via promoting growth transcription and anti-apoptosis genes. It is well known that BET are epigenetic readers which selectively bind to acetylated lysine residues on histone tails and recently BET inhibitor emerged as important therapy in NUT midline carcinoma and several types of hematopoietic cancers [2, 3].
PFI-1 is a potent BET inhibitor and has a similar selectivity with the reported BET inhibitor JQ1. When tested with BEAS-2Bs cells, PFI-1 treatment markedly suppressed the release of IL-6 and CXCL8 induced by IL-1β/H2O2 by inhibiting Brd4 [4]. In leukaemic cell line MV4 which were sensitive to BET inhibitors, PFI-1 treatment induced cell cycle and apoptosis through function on Brd4 [1]. When tested with NET cell lines, administration of PFI-1 reduced cell proliferation by inhibiting BET activity at low concentrations of 100 nM–1 μM [5].
References:
[1]. Picaud, S., et al., PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res, 2013. 73(11): p. 3336-46.
[2]. Perry, M.M., et al., BET bromodomains regulate TGF-beta-induced proliferation and cytokine release in asthmatic airway smooth muscle. J Biol Chem, 2015.
[3]. Yu, L., et al., Small-Molecule BET Inhibitors in Clinical and Preclinical Development and Their Therapeutic Potential. Curr Top Med Chem, 2015.
[4]. Khan, Y.M., et al., Brd4 is essential for IL-1beta-induced inflammation in human airway epithelial cells. PLoS One, 2014. 9(4): p. e95051.
[5]. Kate E Lines, et al., Epigenetic modifiers reduce proliferation of human neuroendocrine tumour cell lines. Endocrine Abstracts, 2013. 31: p149.
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Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.[Pubmed:23095041]
J Med Chem. 2012 Nov 26;55(22):9831-7.
The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The significance of this subset of the epigenetic code is interrogated and interpreted by an acetyllysine-specific protein-protein interaction with bromodomain reader modules. Selective inhibition of the bromo and extra C-terminal domain (BET) family of bromodomains with a small molecule is feasible, and this may represent an opportunity for disease intervention through the recently disclosed antiproliferative and anti-inflammatory properties of such inhibitors. Herein, we describe the discovery and structure-activity relationship (SAR) of a novel, small-molecule chemical probe for BET family inhibition that was identified through the application of structure-based fragment assessment and optimization techniques. This has yielded a potent, selective compound with cell-based activity (PFI-1) that may further add to the understanding of BET family function within the bromodomains.
