BRD 7552PDX1 inducer CAS# 1137359-47-7 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1137359-47-7 | SDF | Download SDF |
| PubChem ID | 23891512 | Appearance | Powder |
| Formula | C33H33N3O15 | M.Wt | 711.63 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (140.52 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | ethyl 4-[[(2R,3R,4S,5R,6S)-4,5-bis(1,3-benzodioxol-5-ylcarbamoyloxy)-2-(hydroxymethyl)-6-methoxyoxan-3-yl]oxycarbonylamino]benzoate | ||
| SMILES | CCOC(=O)C1=CC=C(C=C1)NC(=O)OC2C(OC(C(C2OC(=O)NC3=CC4=C(C=C3)OCO4)OC(=O)NC5=CC6=C(C=C5)OCO6)OC)CO | ||
| Standard InChIKey | AAOLIMLEFKWKOY-IXMSMLDRSA-N | ||
| Standard InChI | InChI=1S/C33H33N3O15/c1-3-43-29(38)17-4-6-18(7-5-17)34-31(39)49-26-25(14-37)48-30(42-2)28(51-33(41)36-20-9-11-22-24(13-20)47-16-45-22)27(26)50-32(40)35-19-8-10-21-23(12-19)46-15-44-21/h4-13,25-28,30,37H,3,14-16H2,1-2H3,(H,34,39)(H,35,40)(H,36,41)/t25-,26-,27+,28-,30+/m1/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 | PDX1 transcription factor inducer; up regulates PDX1 expression in both primary human islets and ductal cells. Induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. Increases insulin expression in PANC-1 cells, primary human islets and human duct-derived cells. |
BRD 7552 Dilution Calculator
BRD 7552 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.4052 mL | 7.0261 mL | 14.0522 mL | 28.1045 mL | 35.1306 mL |
| 5 mM | 0.281 mL | 1.4052 mL | 2.8104 mL | 5.6209 mL | 7.0261 mL |
| 10 mM | 0.1405 mL | 0.7026 mL | 1.4052 mL | 2.8104 mL | 3.5131 mL |
| 50 mM | 0.0281 mL | 0.1405 mL | 0.281 mL | 0.5621 mL | 0.7026 mL |
| 100 mM | 0.0141 mL | 0.0703 mL | 0.1405 mL | 0.281 mL | 0.3513 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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BRD7552 is an inducer of pancreatic and duodenal homeobox 1 (PDX1) [1][2].
PDX1 is a member of the homeodomain-containing transcription factor family. It is a key transcription factor important for both mature β cell function and pancreas development [1]. PDX1 is a master regulatory transcription factor and required for β-cell transdifferentiation [2].
In human cells, BRD7552 upregulated the expression of PDX1 via epigenetically altering PDX1 promoter area [3]. BRD7552 was discovered as a PDX1 inducer in a cell-based phenotypic screening assay. It was used to induce the expression of PDX1. In PANC-1 cells, BRD7552 up-regulated mRNA and protein levels of PDX1. BRD7552 changed epigenetic markers within the PDX1 promoter region that was consistent with transcriptional activation. In cell culture, BRD7552 partially complemented PDX1, enhancing insulin expression induced by the introduction of three genes in PANC-1 cells [2]. In PANC-1 cells, nine-day treatment with BRD7552 dose-dependently increased insulin mRNA expression. In primary human islet cells, three of five donor samples treated with BRD7552 showed significantly dose-dependent induction of PDX1 after 3 or 5 days and of insulin after a 5-day treatment [1]. BRD7552 was capable of inducing the expression of PDX1 in the human PANC-1 ductal cell line [4].
No in vivo application data of this product had been found.
References:
[1]. Yuan Y, Hartland K, Boskovic Z, et al. A small-molecule inducer of PDX1 expression identified by high-throughput screening[J]. Chemistry & biology, 2013, 20(12): 1513-1522.
[2]. Yuan Y. Small-Molecule Modulators of Pancreatic Ductal Cells: Histone Methyltransferases and β-Cell Transdifferentiation [D]. 2013.
[3]. Zhao Y. Developing Therapies with Functional Beta Cells to Treat Diabetes[J]. International Journal of Translational Science, 2015, 1: 41-66.
[4]. Fodor A, Cozma A, Karnieli E. Personalized epigenetic management of diabetes[J]. Personalized Medicine, 2015, 12(5): 497-514.
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A small-molecule inducer of PDX1 expression identified by high-throughput screening.[Pubmed:24290880]
Chem Biol. 2013 Dec 19;20(12):1513-22.
Pancreatic and duodenal homeobox 1 (PDX1), a member of the homeodomain-containing transcription factor family, is a key transcription factor important for both pancreas development and mature beta cell function. The ectopic overexpression of Pdx1, Neurog3, and MafA in mice reprograms acinar cells to insulin-producing cells. We developed a quantitative PCR-based gene expression assay to screen more than 60,000 compounds for expression of each of these genes in the human PANC-1 ductal carcinoma cell line. We identified BRD7552, which upregulated PDX1 expression in both primary human islets and ductal cells, and induced epigenetic changes in the PDX1 promoter consistent with transcriptional activation. Prolonged compound treatment induced both insulin mRNA and protein and also enhanced insulin expression induced by the three-gene combination. These results provide a proof of principle for identifying small molecules that induce expression of transcription factors to control cellular reprogramming.
