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My CartCAS：209984-56-5
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 209984-56-5 |
| Name | Dibenzazepine |
| Molecular Formula | C26H23F2N3O3 |
| Molecular Weight | 463.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD12828734 |
| SMILES | C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)CC4=CC(=CC(=C4)F)F |
| Target Point | Notch;-secretase |
| Passage | Stem Cells;Neuronal Signaling |
| Background | Dibenzazepine is a γ-secretase inhibitor that acts on APPL and Notch cleavage. |
| Biological Activity | YO-01027 (Dibenzazepine;DBZ)是高效的γ-分泌酶抑制剂，裂解Notch和APPL的IC50分别为2.92±0.22和 2.64±0.30 nM。[1-4] |
| IC50 | 2.92±0.22(Notch)，2.64±0.30(APPL)nM[1] |
| In Vitro | 向APPL表达或Notch表达细胞施用的DBZ浓度增加导致APPL CTF片段的逐渐累积和NICD产生的严重剂量依赖性降低[1]。 CE和DBZ的分子靶标是γ-分泌酶复合物中早老素1的N-末端片段[2]。 |
| In Vivo | DBZ阻断来自Ang II输注的Apo E - / - 小鼠和经历AAA修复的人的腹主动脉瘤(AAA)组织中的Notch1信号传导。 DBZ显著阻止Ang II刺激的巨噬细胞和CD4 + T细胞的积聚，以及ERK介导的血管生成，同时在体内逆转Th2反应[3]。 DBZ的施用显著减弱肾纤维化和纤维化标志物的表达，包括胶原1α1/3α1，纤连蛋白和α-平滑肌肌动蛋白。 DBZ显著抑制输尿管梗阻诱导的转化生长因子(TGF)- β，磷酸化Smad 2和Smad 3的表达[4]。 |
| Cell Experiment | 在蛋白质收获前6小时，在诱导Notch或APPL表达后，将DBZ(0.1，1，2.5，5，7.5，10，25，50，100，250nM)加入S2细胞培养基中。对于每个样品，在裂解缓冲液中相应的浓度也包括相同的抑制剂，用于蛋白质提取和免疫印迹分析[1]。 |
| Animal Experiment | 小鼠：在该研究中使用雄性野生型(WT)C57BL / 6J和Apo E - / - 小鼠。在小型泵植入前1天，Ang II处理的小鼠腹膜内注射盐水载体或γ-分泌酶抑制剂，二苯并氮杂(DBZ)(1mg / kg /天，溶于盐水)，并且每天继续治疗4周。使用计算机化的尾套系统在清醒的小鼠中测量血压。将所有小鼠麻醉。移除主动脉组织并准备用于进一步的组织学和分子分析[3]。 |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg 25mg |
是一种γ-secretase抑制剂，作用于APPL和Notch分裂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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