DAPT (GSI-IX)

目录号:S2215 别名: LY-374973

DAPT (GSI-IX) Chemical Structure

Molecular Weight(MW): 432.46

DAPT (GSI-IX)是一种新型γ-secretase抑制剂,抑制 Aβ产生,在HEK 293细胞中IC50为20 nM。

规格 价格 库存 购买数量  
RMB 916.57 现货
RMB 578.14 现货
RMB 984.36 现货
RMB 1715.51 现货
RMB 3028.65 现货
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客户使用该产品的9个实验数据:

  • Int J Cancer, 2018, 142(5):999-1009. DAPT (GSI-IX) purchased from Selleck.

    Western blotting showing increased unconjugated SUMO1 levels in Notch1 ΔE cells treated with 10 uM DAPT for 3 days. Tubulin was used as a loading control.

    Oncogene 2014 10.1038/onc.2014.319. DAPT (GSI-IX) purchased from Selleck.

  • Upper; Effect of DAPT, a Notch inhibitor on Notch4-ICD expression in TAMR-MCF-7 cells. Lower; Effect of DAPT on cell proliferation of TAMR-MCF-7 cells. Cells were exposed to DAPT (0.3-10 μM) and cell proliferation was measured at different time points by MTT assay. Data represent mean ± SD with 6 different samples.

    cancer lett, 2017, 390:115-125. DAPT (GSI-IX) purchased from Selleck.

    Representative E-cadherin staining in MCF-7 and TAMR-MCF-7 cells.

    cancer lett, 2017, 390:115-125. DAPT (GSI-IX) purchased from Selleck.

  • A panel of GICs was treated with the indicated doses of DAPT for 48 hours. γSecretase inhibitors inhibited expression of NICD, Hes1, Hes3, and Hes5 in a dose-dependent manner.

    Stem Cells 2014 32(1), 301-12. DAPT (GSI-IX) purchased from Selleck.

    (E) Western blotting analysis shows DAPT decrease HES1, ALDH1, BMI1 and SOX2 expression in HNSCC CAL27 cell line.

    Sci Rep, 2016, 6:24704. DAPT (GSI-IX) purchased from Selleck.

  • Effects of endosulfan on cytoskeleton and mitosis in HUVECs. Images 7–12 are the 4 × magnified versions of 1–6, respectively. Microfilament (A), microtubule (B), and cell nucleus (C) were incubated with Actin-Tracker Green, Tubulin-Tracker Red, and Hoechst 33258 solution, respectively.

    Environ Pollut, 2017, 221:26-36. DAPT (GSI-IX) purchased from Selleck.

    R26PR;cre tumors express high levels of NICD and are sensitive to pharmacological inhibition of NOTCH1 signaling. (C) A cell line derived from R26PR;MMTV-cre tumor cells was cultured in the presence of a γ-secretase inhibitor, DAPT, or DMSO vehicle. Live cells were counted at 24, 48 and 72 hours of culture. (D) Western blot analysis of NICD following DAPT treatment.

    Dis Model Mech 2013 6(6), 1494-506. DAPT (GSI-IX) purchased from Selleck.

  • Human corneal epithelial cells were subjected to a scratch assay and then treated with DAPT or DMSO (control) (A). The effect of DAPT concentration on scratch assay wound closure rate was measured (P < 0.001) (B).  Western blot for Notch1IC confirmed that 10uM DAPT can effectively inhibit Notch activation (C). HCE-T cells pretreated with DAPT migrated 2.2 times faster than control in transwell migration assay (P < 0.0001) while Jagged1 treated cells migrated 20% slower but did not reach statistical significance (P =0.077) (D).

    Invest Ophth Vis Sci 2012 53,12 . DAPT (GSI-IX) purchased from Selleck.

产品安全说明书

Gamma-secretase抑制剂选择性比较

生物活性

产品描述 DAPT (GSI-IX)是一种新型γ-secretase抑制剂,抑制 Aβ产生,在HEK 293细胞中IC50为20 nM。
特性 DAPT(GSI-IX)是新型γ-分泌酶抑制剂。
靶点
γ secretase(Aβ) [1]
(HEK 293 cells)
20 nM
体外研究

DAPT功能性抑制γ-分泌酶而降低HEK 293细胞中全部Aβ产量,IC50为20 nM。DAPT作用于原代培养的人神经细胞,也抑制Aβ产量,作用于全部Aβ和Aβ42时, IC50分别为115 nM和200 nM,比作用于HEK 293细胞时低5-10倍。最新研究显示DAPT 抑制SK-MES-1 细胞增殖,这种作用存在浓度依赖性,IC50为11.265 μM。此外, DAPT作用于肺鳞状细胞癌细胞,通过抑制Notch受体信号通路,也诱导依赖型和非依赖型细胞凋亡。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 CD133− NVX1S2Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[yJO69VQ>? NH\MUXE1QCCq MVLlcohidmOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGmwZIXj[YQh[nliQ1TEVC=> MVmyOFUxOjl2OR?=
A549 CD133+ M1vBbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKyJO69VQ>? NYH0ZVBkPDhiaB?= M17VXYVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7keYNm\CCkeTDDSGRR NIDPdZUzPDVyMkm0PS=>
HT29  NHfZVmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnCZZI1OC53LUe1JO69VQ>? MnPpNVIwOjRxNEigbC=> NVqxUIpxTE2VTx?= NY\DVmtPcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiY3;uZ4VvfHKjdHnvckBu[W6wZYK= NG\BW4YzPTJ3N{m0OS=>
SHG-44 NXToUmNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PhUVAvPS1zMDFOwG0> NXXYSpMzOS13IHS= NGLPSZRqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkh[XRidHjlJI9xfGmvYXygZ49v[2WwdILheIlwdiCxZjCxJO69VQ>? MX2yOVA3OzJ6NR?=
MG63 MojmSpVv[3Srb36gRZN{[Xl? NH;O[VAyODBizszN Mn;jNlQhcA>? NIKzPXlFVVOR M{fJT4Rme2Wwc3n0bZpmeyC2aHWgZ4VtdCCuaX7lJJRwKGOrc4DsZZRqdiC2cnXheI1mdnR? MnjGNlQ5QTR{OUe=
Saos-2 MoLGSpVv[3Srb36gRZN{[Xl? NHXYO48yODBizszN Mlm0NlQhcA>? MULEUXNQ NYD5Ums6\GW|ZX7zbZRqgmW|IITo[UBk\WyuIHzpcoUhfG9iY3nzdIxifGmwIITy[YF1dWWwdB?= MYiyOFg6PDJ7Nx?=
U251 MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGKwUFMzKM7:TR?= M{jadlQ5KGh? MmjESG1UVw>? NYG0bXI4e3S{ZX7neIhmdnQEoIStRXVESi2rbnT1Z4VlKGOnbHyg[5Jwf3SqIIP1dJBz\XO|aX;u MViyOFc6OzNzMx?=
U87  M{LmbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvmVJEzKM7:TR?= MlT3OFghcA>? NX\We4hFTE2VTx?= M2r5Z5N1emWwZ4To[Y5{yqC2LVHVR2IucW6mdXPl[EBk\WyuIHfyc5d1cCC|dYDwdoV{e2mxbh?= M3G0OFI1Pzl|M{Gz
U251 MX7GeY5kfGmxbjDBd5NigQ>? NIDXSFYzKM7:TR?= NV;VT3pDPDhiaB?= M1\XUWROW09? NVH6XWRy[myxY3vzxsB1NUGXQ1KtbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKHSqZTDwN|ghVUGSSz;NRXBMSVCNMj;Id5AzPyCyYYToe4F6KGGwZDDpcohq[mm2czDlfJBz\XO|aX;uJI9nKE6LQ1Sx MUKyOFc6OzNzMx?=
U87  MYXGeY5kfGmxbjDBd5NigQ>? MUKyJO69VQ>? NXfPZ2lXPDhiaB?= M3vBOmROW09? M{HNUoJtd2Otc9MgeE1CXUOELXnu[JVk\WRiYXP0bZZifGmxbjDv[kB1cGVicEO4JG1CWEtxTVHQT2FRUzJxSIPwNlcheGG2aIfhfUBidmRiaX7obYJqfHNiZYjwdoV{e2mxbjDv[kBPUUOGMR?= MlX1NlQ4QTN|MUO=
A549  MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XkUlExKM7:TR?= MlvaNlRp M2HOc4Rm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkh[2:vYnnu[YQhf2m2aDDQWGU> M3PrWFI{PjdzNkG5
GC-B  MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\kVXU3NjJ3LUGwNEDPxE1? MXKyOEBp MU\EUXNQ NGj3[ItqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M2\Oc|E6PTR{NES2

... Click to View More Cell Line Experimental Data

体内研究 DAPT按100mg/kg剂量处理PDAPP小鼠,产生强劲和持久的药效,1小时内脑中 DAPT水平超过100 ng/g ,且处理后,持续上升达18小时,3小时后的时候观察到最高水平为490 ng/g。在此期间, DAPT 按100 mg/kg剂量处理,也降低大脑皮层全部Aβ和Aβ42,这种作用存在剂量依赖性,降低50%。[1] DAPT按40 mg/kg剂量作用于大鼠大脑皮层, 抑制LPS诱导的γ分泌酶活性,且提高携带长期神经炎症的细胞凋亡。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

体外Aβ减少检测实验 :

转染APP751(HEK 293)基因的人类胚胎肾细胞,用于常规 Aβ减少检测。细胞接种在96孔板上,在含10%热灭活胎牛血清的DMEM培养基上粘附过夜。 DAPT 在 DMSO中稀释,终浓度为0.1% DMSO。使用DAPT在37oC下预处理细胞2小时,吸除培养基,使用新鲜实验化合物溶液。再处理2小时后,抽除条件培养基,使用标准 ELISA(266-3D6)分析全部Aβ。根据使用 0.1% DMSO 处理的对照组细胞,测量Aβ产量的减少,表示为抑制百分数。实验至少按6种剂量重复进行,得到实验数据,然后使用XLfit软件拟合四参数方程,测定 药性。培养的人和PDAPP小鼠神经细胞在无血清培养基上生长,增强他们的神经元特性,其中有90%以上神经元在实验使用前成熟。通过在每孔中加入新鲜培养基,然后在没有DAPT存在时,在37oC下温育24小时,收集条件培养基中得到的基底Aβ值。使用含DAPT的新鲜培养基,按所需浓度范围在37oC下再处理培养细胞24小时,收集条件培养基。为了测量全部Aβ,使用与HE2K 293细胞实验 相同的ELISA(266-3D6) 分析样本。通过分开的ELISA(21F12-3D6),使用特定Aβ42 C-端捕获抗体,进行Aβ42 产量分析。测定对全部Aβ和Aβ42产量的抑制情况。绘制与DAPT浓度相对的抑制百分数,使用 XLfit 软件分析数据,测定药性。
细胞实验:[2]
+ 展开
  • Cell lines: SK-MES-1
  • Concentrations: 2.5 μM到 160 μM
  • Incubation Time: 72小时
  • Method: 细胞接种在96孔板上,使用0.1% DMSO或 DAPT(浓度为2.5 μM-160 μM )处理72小时。使用MTT染料减少检测实验,稍微修正,测定细胞毒性。与DAPT温育后, 20 μL MTT溶液 (5 mg/mL,溶于 PBS)加到含 180 μL培养基的每孔中,实验板在37 oC下温育4小时,随后每孔加入150 μL DMSO,在室温下震荡15分钟混合。通过酶联免疫吸附法在490 nm处测定吸光值。使用α-MEM 及等量的MTT 溶液和溶剂,作为空白对照。使用PROBIT 程序在SPSS中计算IC50值。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 过表达淀粉样前体蛋白APPV717F 突变型的杂合PDAPP转基因小鼠
  • Formulation: DAPT溶于玉米油, 5% (v/v) 乙醇中
  • Dosages: ≤100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 86 mg/mL (198.86 mM)
Ethanol 50 mg/mL (115.61 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+corn oil
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 432.46
化学式

C23H26F2N2O4

CAS号 208255-80-5
稳定性 powder
in solvent
别名 LY-374973

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03461484 Active not recruiting Coronary Artery Stenoses|Stable Angina|Ischemia|NSTEMI - Non-ST Segment Elevation MI|STEMI Biosensors Europe SA|European Cardiovascular Research Center March 6 2014 --
NCT03023020 Recruiting High Bleeding Risk|Coronary Artery Disease|PCI ECRI bv|Cardialysis B.V.|European Cardiovascular Research Center|University of Bern|Terumo Medical Corporation April 4 2017 Not Applicable
NCT02798913 Unknown status Peripheral Artery Disease Federico II University January 2016 Phase 3
NCT02609698 Recruiting Stable Angina Unstable Angina Silent Coronary Ischemia Coronary Artery Disease Ajou University School of Medicine|B. Braun Korea Co. Ltd. August 2015 Phase 4
NCT02516267 Recruiting Bleeding University of Sao Paulo General Hospital July 2015 Not Applicable
NCT01459627 Completed Myocardial Infarction|Cardiovascular Disease Maasstad Hospital|Medtronic December 2011 Phase 4

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操作手册

如果有其他问题,请给我们留言。

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常见问题及建议解决方法

  • 问题 1:

    Could you please help test the formulation of S2215 for in vivo studies?

  • 回答:

    S2215 DAPT in 30% PEG400+0.5% Tween80+5% Propylene glycol at 10 mg/ml is a suspension. We tried to add some EtOH, and it dissolved clearly in organice solvents, but when water added, the precipitation went out immediately. Then we tried other vehicles, and found S2215 can be dissolved in 4% DMSO+corn oil at 10 mg/ml clearly.

  • 问题 2:

    I would like to ask if you would recommend this product used in endothelial cells (e.g. both murine and human endothelial cells).

  • 回答:

    I think DAPT can be used in endothelial cells from both human and mouse, please see the following reference: http://www.ncbi.nlm.nih.gov/pubmed/19481797; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2615564/

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID