For research use only. Not for therapeutic Use.
BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function[1].
BRD7552 (0-5 μM; 5 days) induces a dose-dependent increase in PDX1 protein levels after BRD7552 treatment in PANC-1 cells[1].
BRD7552 acts in a FOXA2-dependent manner to increase PDX1 expression in human ductal cells. Nine-day treatment of PANC-1 cells with BRD7552 (0-10 μM) causes a dose-dependent increase in insulin mRNA expression. BRD7552 induces insulin expression in PANC-1 cells. BRD7552 increases H3 acetylation and H3K4me3 and decreases H3K9me3, results that are consistent with transcriptional activation of PDX1. The epigenetic changes induced by BRD7552 are consistent with transcriptional activation, and BRD7552 acts in a FOXA2-dependent manner[1].
| Catalog Number | I000518 |
| CAS Number | 1137359-47-7 |
| Synonyms | ethyl 4-[[(2R,3R,4S,5R,6S)-4,5-bis(1,3-benzodioxol-5-ylcarbamoyloxy)-2-(hydroxymethyl)-6-methoxyoxan-3-yl]oxycarbonylamino]benzoate |
| Molecular Formula | C33H33N3O15 |
| Purity | ≥95% |
| 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 |
| InChIKey | AAOLIMLEFKWKOY-IXMSMLDRSA-N |
| 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 |
| Reference | [1]. Yuan Y, et al. A small-molecule inducer of PDX1 expression identified by high-throughput screening [published correction appears in Chem Biol. 2014 Feb 20;21(2):306]. Chem Biol. 2013;20(12):1513-1522. |
