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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥545.00 | 现货 | |
10mg | ¥750.00 | 现货 | |
50mg | ¥2250.00 | 现货 |
特色产品
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- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
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- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
DAPT,N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester,是一种有效的、特异性的γ分泌酶抑制剂。γ分泌酶是一个多聚膜蛋白复合体,催化淀粉样前体蛋白(APP)的水解,从而导致β淀粉样蛋白(Aβ)的积累,其与家族性阿尔兹海默病(AD)的早期症状相关联。DAPT直接结合γ分泌酶催化中心的C端片段,即presenilin (PS),尤其是第7个跨膜结构域或更大的C-末端区域,从而合成一个光活化的DAPT衍生物。
在幼年(6个月大,无斑块)和老年(17个月大,有斑块)Tg2576小鼠中,DAPT口服给药可以剂量依赖性的减少血浆和脑脊液中Aβ肽的水平。
参考文献:
Thomas A. Lanz, Carol S. Himes, Giovanni Pallante, Lisa Adams, Shinji Yamazaki, Ben Amore, and Kalpana M. Merchant. The γ-secretase inhibitor N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester reduces Aβ levels in vivo in plasma and cerebrospinal fluid in young (plague-free) and aged (plaque-bearing) Tg2576 mice. The Journal of Pharmacology and Experimental Therapeutics 2003: 305 (3) 864-871
Yuichi Morohashi, Toshiyuki Kan, Yusuke Tominari, Haruhiko Fuwa, Yumiko Okamura, Naoto Watanabe, Chihiro Sato, Hideaki Natsugari, Tohru Fukuyama, Takeshi Iwatsubo, and Taisuke Tomita. C-terminal fragment of presenilin is the molecular target of a dipeptidic γ-secretase-specific inhibitor DAPT (N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylg
-lycine t-butyl Ester). The Journal of Biological Chemistry 2006: 281(21) 14670-14676
产品性质
物理外观 | A solid |
CAS号 | 208255-80-5 |
分子式 | C23H26F2N2O4 |
分子量 | 432.46 |
小分子别名 | DAPT |
化学名称 | tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate |
溶解度 | ≥21.62 mg/mL in DMSO; insoluble in H2O; ≥16.36 mg/mL in EtOH with ultrasonic |
SMILES | CC(C(=O)NC(C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
生物活性描述 | DAPT (GSI-IX)是一种新型的γ分泌酶抑制剂,在HEK 293细胞中的IC50值为20 nM。 |
靶点 | Aβ |
生物活性数据 | 20 nM |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. Julia Sidor, Megan Gillette, et al. "Role of Presenilin-1 in Aggressive Human Melanoma." Int J Mol Sci. 2022 Apr 28;23(9):4904. PMID: 35563300
- 2. Xiaoya An, Guoliang Wang, et al. "Novel cell culture paradigm prolongs mouse corneal epithelial cell proliferative activity in vitro and in vivo." Front Cell Dev Biol. 2021 Jun 30;9:675998. PMID: 34277619
- 3. Shanfeng Sun, Songsong Jiang, et al. "Cholera toxin induces food allergy through Th2 cell differentiation which is unaffected by Jagged2." Life Sci. 2020 Oct 1;263:118514. PMID: 33010283
- 4. Weigang He, Jinxia Sun, et al. "Andrographolide exerts anti‐inflammatory effects in Mycobacterium tuberculosis‐infected macrophages by regulating the Notch1/Akt/NF‐κB axis." J Leukoc Biol. 2020 Dec;108(6):1747-1764. PMID: 32991757
- 5. Shu min Lv, Hongwen Cai, et al. "Thymosin‑β 4 induces angiogenesis in critical limb ischemia mice via regulating Notch/NF‑κB pathway." Int J Mol Med. 2020 Oct;46(4):1347-1358. PMID: 32945357
- 6. Ireland AS, Micinski AM, et al. "MYC Drives Temporal Evolution of Small Cell Lung Cancer Subtypes by Reprogramming Neuroendocrine Fate." Cancer Cell. 2020 Jul 13;38(1):60-78.e12. PMID: 32473656
- 7. Zhu M, Li Y, et al. "Effects of bisphenol A and its alternative bisphenol F on Notch signaling and intestinal development: A novel signaling by which bisphenols disrupt vertebrate development." Environ Pollut. 2020;263(Pt B):114443. PMID: 32311622
- 8. Zhu M, Niu Y, et al. "Low Concentrations of Tetrabromobisphenol A Disrupt Notch Signaling and Intestinal Development in in Vitro and in Vivo Models." Chem Res Toxicol. 2020;10.1021/acs.chemrestox.9b00528. PMID: 32041402
- 9. Jennifer E. Speer, Yuli Wang, et al. "Evaluation of human primary intestinal monolayers for drug metabolizing capabilities." Journal of Biological Engineering volume 13, Article number: 82 (2019)
- 10. Wu J, Wang X, et al. "Allyl isothiocyanate may reverse the expression of MRP1 in COPD rats via the Notch1 signaling pathway." Arch Pharm Res. 2019 Sep 30. PMID: 31571144
- 11. Speer JE, Gunasekara DB, et al. "Molecular transport through primary human small intestinal monolayers by culture on a collagen scaffold with a gradient of chemical cross-linking." J Biol Eng. 2019 Apr 27;13:36. PMID: 31061676
- 12. Azimi M, Brown NL. "Jagged1 protein processing in the developing mammalian lens." Biol Open. 2019 Mar 26;8(3). pii: bio041095. PMID: 30890522
- 13. Wu F, Wu D, et al. "Generation of hepato-biliary organoids from human induced pluripotent stem cells." J Hepatol. 2019 Jan 7. pii: S0168-8278(19)30002-9. PMID: 30630011
- 14. MXinwei Feng, Junfeng Lu, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
- 15. Tang J, Zhou H, et al. "Dual-Mode Imaging-Guided Synergistic Chemo- and Magnetohyperthermia Therapy in a Versatile Nanoplatform To Eliminate Cancer Stem Cells." ACS Appl Mater Interfaces.2017 Jul 19;9(28):23497-23507. PMID: 28661121
- 16. Fan Y, Gao X, Chen J, et al. "HIV Tat Impairs Neurogenesis through Functioning As a Notch Ligand and Activation of Notch Signaling Pathway." J Neurosci. 2016 Nov 2;36(44):11362-11373. PMID: 27807176
- 17. Zhou, Xuanxuan, et al. "Tetrahydroxystilbene glucoside extends mouse lifespan via up-regulating neural Klotho and down-regulating neural insulin/insulin-like growth factor 1." Neurobiology of Aging (2014).