GSK 5959Potent and selective BRPF1 inhibitor CAS# 901245-65-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 901245-65-6 | SDF | Download SDF |
| PubChem ID | 15990224 | Appearance | Powder |
| Formula | C22H26N4O3 | M.Wt | 394.47 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 13 mg/mL (32.96 mM; Need ultrasonic and warming) | ||
| Chemical Name | N-(1,3-dimethyl-2-oxo-6-piperidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide | ||
| SMILES | CN1C2=CC(=C(C=C2N(C1=O)C)N3CCCCC3)NC(=O)C4=CC=CC=C4OC | ||
| Standard InChIKey | LTUGYAOMCKNTGG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27) | ||
| 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 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3. Cell permeable. |
GSK 5959 Dilution Calculator
GSK 5959 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.535 mL | 12.6752 mL | 25.3505 mL | 50.7009 mL | 63.3762 mL |
| 5 mM | 0.507 mL | 2.535 mL | 5.0701 mL | 10.1402 mL | 12.6752 mL |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.535 mL | 5.0701 mL | 6.3376 mL |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.507 mL | 1.014 mL | 1.2675 mL |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.507 mL | 0.6338 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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Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and beta2-adrenoceptor agonist properties.[Pubmed:25100753]
J Pharmacol Exp Ther. 2014 Oct;351(1):190-9.
The objective of the present studies was to characterize the pharmacologic properties of GSK-961081 [TD-5959; (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)et hyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl) piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate], a novel first-in-class inhaled bifunctional compound possessing both muscarinic antagonist (MA) and beta2-adrenoceptor agonist (BA) properties (MABA). In competition radioligand binding studies at human recombinant receptors, GSK-961081 displayed high affinity for hM2 (Ki = 1.4 nM), hM3 muscarinic receptors (Ki = 1.3 nM) and hbeta2-adrenoceptors (Ki = 3.7 nM). GSK-961081 behaved as a potent hbeta2-adrenoceptor agonist (EC50 = 0.29 nM for stimulation of cAMP levels) with 440- and 320-fold functional selectivity over hbeta1- and hbeta3-adrenoceptors, respectively. In guinea pig isolated tracheal tissues, GSK-961081 produced smooth muscle relaxation through MA (EC50 = 50.2 nM), BA (EC50=24.6 nM), and MABA (EC50 = 11 nM) mechanisms. In the guinea pig bronchoprotection assay, inhaled GSK-961081 produced potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED50 = 33.9 microg/ml), BA (ED50 = 14.1 microg/ml), and MABA (ED50 = 6.4 microg/ml) mechanisms. Significant bronchoprotective effects of GSK-961081 were evident in guinea pigs via MA, BA, and MABA mechanisms for up to 7 days after dosing. The lung selectivity index of GSK-961081 in guinea pigs was 55- to 110-fold greater than that of tiotropium with respect to systemic antimuscarinic antisialagogue effects and was 10-fold greater than that of salmeterol with respect to systemic beta2-adrenoceptor hypotensive effects. These preclinical findings studies suggest that GSK-961081 has the potential to be a promising next-generation inhaled lung-selective bronchodilator for the treatment of airway diseases, including chronic obstructive pulmonary disease.
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.
