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DAPT (GSI-IX)γ分泌酶抑制剂

DAPT (GSI-IX)

产品编号:A8200
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10mM (in 1mL DMSO) ¥600.00 现货
10mg ¥700.00 现货
50mg ¥2,600.00 现货
500mg ¥9,800.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. 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
2. 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.
3. 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
4. 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
5. 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).

质量控制

化学结构

DAPT

相关生物数据

DAPT
The result shows the level of Aβ40 and Aβ42 decreased as the DAPT concentration increased. Compared with Aβ42, the level of Aβ420 decreased more rapidly with increasing DAPT concentration.

相关生物数据

DAPT
The Neuro-2A cells (transfected with Klotho) were treated with DAPT for 16 h. The transfected Neuro-2A without DAPT treatment was assigned as control. Un-transfected Neruo-2A was assigned as wild type cells (wt). The protein levels of Klotho and Klotho (sub) from cells lysate were analyzed using Klotho and Flag antibody respectively. Gamma-secretase inhibitor DAPT could cleave Klotho stub. After treatment with DAPT, 5 kDa fragment was found in transfected cells, which was not seen in wt and control group.

相关生物数据

DAPT

相关生物数据

DAPT

相关生物数据

DAPT

相关生物数据

DAPT

相关生物数据

DAPT

DAPT (GSI-IX) Dilution Calculator

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化学性质

CAS号 208255-80-5 SDF Download SDF
别名 gamma-Secretase Inhibitor IX, DAPT, GSI-IX
化学名 tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate
SMILES CC(C(=O)NC(C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
分子式 C23H26F2N2O4 分子量 432.46
溶解度 ≥21.623mg/mL in DMSO 储存条件 Store at 4°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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          
IC50 20 nM          

实验操作

细胞实验[1]:

细胞系

SHG-44人脑胶质瘤细胞系

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

5天;1.0 μM

应用

与A组(对照组)相比,DAPT抑制了B(0.5 μM)、C(1 μM)、D(5 μM)和E(10 μM)组SHG-44细胞的增殖。B组和A组的结果具有显著差异(P<0.05)。然而,B组的细胞活力显著高于C、D和E组(P<0.05)。结果表明,逐渐增加的抑制效应与逐渐增加的DAPT浓度相关。然而,在C、D和E组之间没有差异(P>0.05)。DAPT是一种浓度依赖性的抑制剂,可明显抑制SHG-44细胞的增殖。当浓度高于1.0 μmol/L时,其对细胞的抑制作用没有明显的差异,因而1.0 μmol/L是我们优先考虑的浓度。

动物实验[2]:

动物模型

雄性Balb/C小鼠

剂量

10 mg/kg/day;皮下注射

应用

CT26结肠腺癌细胞(5×105)悬浮在500 μL的磷酸盐缓冲液(PBS)中,皮下接种到所有小鼠的背部。DAPT显著减少血清sVEGFR1,然而无法改变对照小鼠血清中VEGF的浓度。肿瘤的免疫组化研究表明,DAPT减少CD31阳性细胞的数量(280.6 ± 81 vs. 386 ± 59.9 CD31阳性细胞/mm2),尽管在统计学上是不显著的。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Liu X, Xu Q R, Xie W F, et al. DAPT suppresses the proliferation of human glioma cell line SHG-44[J]. Asian Pacific journal of tropical medicine, 2014, 7(7): 552-556.

[2] Kalantari E, Saeidi H, Kia N S, et al. Effect of DAPT, a gamma secretase inhibitor, on tumor angiogenesis in control mice[J]. Advanced biomedical research, 2013, 2.

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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