YO-01027 (Dibenzazepine, DBZ)γ-secretase inhibitor CAS# 209984-56-5 |
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Quality Control & MSDS
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| Cas No. | 209984-56-5 | SDF | Download SDF |
| PubChem ID | 11454028 | Appearance | Powder |
| Formula | C26H23F2N3O3 | M.Wt | 463.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Dibenzazepine; DBZ | ||
| Solubility | DMSO : ≥ 33 mg/mL (71.20 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide | ||
| SMILES | CC(C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)CC4=CC(=CC(=C4)F)F | ||
| Standard InChIKey | QSHGISMANBKLQL-OWJWWREXSA-N | ||
| Standard InChI | InChI=1S/C26H23F2N3O3/c1-15(29-23(32)13-16-11-17(27)14-18(28)12-16)25(33)30-24-21-9-4-3-7-19(21)20-8-5-6-10-22(20)31(2)26(24)34/h3-12,14-15,24H,13H2,1-2H3,(H,29,32)(H,30,33)/t15-,24-/m0/s1 | ||
| 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 | YO-01027 (Dibenzazepine, DBZ) is a dipeptidic inhibitor of γ-secretase with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively. | |||||
| Targets | APPL | Notch | ||||
| IC50 | 2.6 nM | 2.9 nM | ||||
YO-01027 (Dibenzazepine, DBZ) Dilution Calculator
YO-01027 (Dibenzazepine, DBZ) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1576 mL | 10.788 mL | 21.5759 mL | 43.1518 mL | 53.9398 mL |
| 5 mM | 0.4315 mL | 2.1576 mL | 4.3152 mL | 8.6304 mL | 10.788 mL |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1576 mL | 4.3152 mL | 5.394 mL |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 0.863 mL | 1.0788 mL |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.4315 mL | 0.5394 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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YO-01027, also known as dibenzazepine or DBZ, is a potent inhibitor of γ-secretase, a multisubunit aspartyl protease catalyzing the cleavage of numerous type I integral membrane proteins (such as amyloid precursor protein (APP) and Notch). YO-01027 also potently blocks amyloid precursor protein-like (APPL) and Notch cleavage, with estimated inhibition constant IC50 of 2.640.30 nM and 2.920.22 nM respectively, through interaction with the N-terminal fragment of Presenilin in a dose-response manner. Recent studies show that YO-01027-induced inhibition Notch signaling pathway leads to a rapid conversion of proliferative crypt cells into postmitotic cells and impairs MUC16 biosynthesis in a concentration-dependent manner in undifferentiated cells instead of postmiotic stratified cells at both preconfluent and confluent stages.
Reference
Linjie Xiong, Ashley M. Woodward, and Pablo Argueso. Notch signaling modulates MUC16 biosynthesis in an vitro model of human corneal and conjunctival epithelial cell differentiation. Invest. Ophthalmol. Vis. Sci. 2011, 52(8), 5641-5646
Casper Groth, W. Gregory Alvord, Octavio A. Quinones, and Mark E. Fortini. Pharmacological analysis of drosphila melanogaster γ-secretase with respect to differential proteolysis of Notch and APP. Mol. Pharmacol. 2010, 77(4), 567-574
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YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.
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