Product Description
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively. YO-01027 targets the Presenilin fragment. Increasing concentrations of YO-01027 administered to APPl- or Notch-expressing cells leads to the progressive accumulation of APPL C-terminal fragments and a decrease in NICD production in a dose-dependent manner. [1] In an in vitro model of human corneal and conjunctival epithelial cell differentation, YO-01027 impaired MUC16 biosynthesis in a concentration-dependent manner. [2]In oncology models, YO-01027 preferentially inhibited Notch and significantly decreased MCF7 tumors and increased latency compared with control mice. [3]
Technical information:
| Chemical Formula: | C26H23F2N3O3 | |
| CAS #: | 209984-56-5 | |
| Molecular Weight: | 463.48 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | 7-(S)-[N(3,5-difluorophenylacetyl)-L-alaninyl]amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | YO-01027, YO01027, Dibenzazepine, Deshydroxy LY 411575 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Groth et al., Pharmacological Analysis of Drosophila melanogaster g-Secretase with Respect to Differential Proteolysis of Notch and APP. Mol. Pharmacol. 2010, 77(4), 567-574. Pubmed ID: 20064975 |
| 2. | Xiong et al., Notch Signaling Modulates MUC16 Biosynthesis in an In Vitro Model of Human Corneal and Conjunctival Epithelial Cell Differentiation. Invest. Ophthalmol. Vis. Sci. 2011, 52(8), 5641-5646. Pubmed ID: 21508102 |
| 3. | Harrison et al., Regulation of Breast Cancer Stem Cell Activity by Signaling through the Notch4 Receptor. Cancer Res., 2010, 70, 709-718. Pubmed ID: 20068161 |
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