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Catalog No. A8200

DAPT (GSI-IX)（别名：DAPT）

γ分泌酶抑制剂

规格	价格	库存
1mL(10 mM in DMSO)	￥545.00	现货
10mg	￥750.00	现货
50mg	￥2250.00	现货

CAS号：208255-80-5纯度：99.08%

仅用于科研，不用于诊疗。未经明确授权不得转售。

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特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phosbind Acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 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

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 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

HotStart™ 2X SYBR Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

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

请选择批次查看:

纯度 = 98.20%

COA (Certificate Of Analysis)HPLC NMR (Nuclear Magnetic Resonance)MSDS (Material Safety Data Sheet)

操作说明

Datasheet

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).