产品描述: | YO-01027 (Dibenzazepine) (GMP) is YO-01027 (HY-13526) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. YO-01027 is a potent γ-secretase inhibitor |
靶点: |
IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM;Gamma-secretase |
体内研究: |
DBZ blocks activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E-/- mice and human undergoing AAA repair. DBZ markedly prevents Ang II-stimulated accumulation of macrophages and CD4+ T cells, and ERK-mediated angiogenesis, simultaneously reverses Th2 response, in vivo. Administration of DBZ markedly attenuates renal fibrosis and expression of fibrotic markers, including collagen 1α1/3α1, fibronectin, and α-smoothmuscle actin. DBZ significantly inhibits ureteral obstruction -induced expression of transforming growth factor (TGF)- β, phosphorylated Smad 2, and Smad 3 |
参考文献: |
1. Groth C, et al. Pharmacological analysis of Drosophila melanogaster gamma-secretase with respect to differential proteolysis of Notch and APP. Mol Pharmacol. 2010 Apr;77(4):567-74. 2. Fuwa H, et al. Divergent synthesis of multifunctional molecular probes to elucidate the enzyme specificity of dipeptidic gamma-secretase inhibitors. ACS Chem Biol. 2007 Jun 15;2(6):408-18. 3. Zheng YH, et al. Notch γ-secretase inhibitor dibenzazepine attenuates angiotensin II-induced abdominal aortic aneurysm in ApoE knockout mice by multiple mechanisms. PLoS One. 2013 Dec 16;8(12):e83310. 4. Xiao Z, et al. The Notch γ-secretase inhibitor ameliorates kidney fibrosis via inhibition of TGF-β/Smad2/3 signaling pathway activation. Int J Biochem Cell Biol. 2014 Oct;55:65-71. |
溶解性: |
DMSO : 50 mg/mL (107.88 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.158 ml |
10.788 ml |
21.576 ml |
5 mM |
0.432 ml |
2.158 ml |
4.315 ml |
10 mM |
0.216 ml |
1.079 ml |
2.158 ml |
50 mM |
0.043 ml |
0.216 ml |
0.432 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |