DAPT
Cat. No.：YN380070
| 产品名称: | DAPT |
| CAS No.: | 208255-80-5 |
| Chemical Name: | N-[2S-(3,5-difluorophenyl)acetyl]-L-alanyl-2-phenyl-glycine, 1,1-dimethylethyl ester |
| Synonyms: | GSI-IX |
| 分子量: | 432.46 |
| 分子式: | C₂₃H₂₆F₂N₂O₄ |
| SMILES: | FC1=CC(F)=CC(CC(N[C@H](C(N[C@H](C(OC(C)(C)C)=O)C2=CC=CC=C2)=O)C)=O)=C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | DAPT (GSI-IX) 是一种有效的，口服活性的 γ 分泌酶 (γ-secretase) 抑制剂，对总amyloid-β (Aβ)和Aβ42的IC50分别为 115 nM 和 200 nM。DAPT 抑制Notch 1信号传导并诱导细胞分化。DAPT 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)。DAPT 具有神经保护活性，并可用于自身免疫性和淋巴增生性疾病，退化性疾病和癌症的研究。 |
| IC50和靶点: | |
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Dovey, H.F., John, V., Anderson, J.P., et al.Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brainJ. Neurochem.76(1),173-181(2001)
Portelius, E., Zhang, B., Gustavsson, M.K., et al.Effects of γ-secretase inhibition on the amyloid β isoform pattern in a mouse model of Alzheimer's diseaseNeurodegener.Dis.6,258-262(2009)
El Mouedden, M., Vandermeeren, M., Meert, T., et al.Reduction of Aβ levels in the Sprague Dawley rat after oral administration of the functional γ-secretase inhibitor, DAPT: A novel non-transgenic model for Aβ production inhibitorsCurr. Pharm. Des.12,671-676(2006)
Kanungo, J., Zheng, Y.L., Amin, N.D., et al.The Notch signaling inhibitor DAPT down-regulates cdk5 activity and modulates the distribution of neuronal cytoskeletal proteinsJ. Neurochem.106,2236-2248(2008)
De Smedt, M., Hoebeke, I., Reynvoet, K., et al.Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironmentBlood106(10),3498-3506(2005)
