DAPT (GSI-IX)

For research use only. Not for use in humans.

製品コードS2215 別名:LY-374973

DAPT (GSI-IX)化学構造

分子量(MW):432.46

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 20500 あり
JPY 13600 あり
JPY 21900 あり
JPY 36800 あり
JPY 63400 あり
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バルク問合せ

文献中Selleckの製品使用例(220)

製品安全説明書

Gamma-secretase阻害剤の選択性比較

生物活性

製品説明 DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.
ターゲット
γ secretase(Aβ) [1]
(HEK 293 cells)
20 nM
体外試験

In human primary neuronal cultures, DAPT also shows inhibitory effects on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ total and Aβ42, which is 5-10-fold lower than is observed in HEK 293 cells. [1] A recent study shows that DAPT inhibits the proliferation of SK-MES-1 cells in a concentration-dependent manner with IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and caspase-independent apoptosis in lung squamous cell carcinoma cells by inhibiting Notch receptor signaling pathway. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 CD133− M{DWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnKZWlHOiEQvF2= NX\nWmJsPDhiaB?= M4Doc4VvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7keYNm\CCkeTDDSGRR MVeyOFUxOjl2OR?=
A549 CD133+ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPmNkDPxE1? NXPXRXM6PDhiaB?= NFzOO3hmdmijbnPld{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnu[JVk\WRiYomgR2RFWA>? M3L4ZlI1PTB{OUS5
HT29  MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfjbpRGOC53LUe1JO69VQ>? MmPPNVIwOjRxNEigbC=> M3GzPGROW09? M2TOcIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGOxbnPlcpRz[XSrb36gcYFvdmW{ MYiyOVI2Pzl2NR?=
SHG-44 MluwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HrWlAvPS1zMDFOwG0> NVrLNlRbOS13IHS= NXT5NmhLcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGG2IITo[UBweHSrbXHsJINwdmOnboTyZZRqd25ib3[gNUDPxE1? NGDxR4szPTB4M{K4OS=>
MG63 NITSZXhHfW6ldHnvckBCe3OjeR?= M4WzNlExOCEQvF2= NEnuOJYzPCCq M3nTdmROW09? NUTERW4y\GW|ZX7zbZRqgmW|IITo[UBk\WyuIHzpcoUhfG9iY3nzdIxifGmwIITy[YF1dWWwdB?= MWWyOFg6PDJ7Nx?=
Saos-2 NIr5OVVHfW6ldHnvckBCe3OjeR?= MVexNFAh|ryP NGfkVokzPCCq NUjrdnFsTE2VTx?= MWHk[ZNmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZTD0c{BkcXOybHH0bY4hfHKnYYTt[Y51 MlT2NlQ5QTR{OUe=
U251 MljxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGyJO69VQ>? NG\WcJQ1QCCq Mo\ySG1UVw>? M2[wSpN1emWwZ4To[Y5{yqC2LVHVR2IucW6mdXPl[EBk\WyuIHfyc5d1cCC|dYDwdoV{e2mxbh?= NGDye3EzPDd7M{OxNy=>
U87  M4PUWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jzVVIh|ryP M{HjWVQ5KGh? NEnPOYJFVVOR NF2zbIN{fHKnbnf0bIVve8LidD3BWWNDNWmwZIXj[YQh[2WubDDndo94fGhic4XwdJJme3Orb36= MYKyOFc6OzNzMx?=
U251 NH7jZWVHfW6ldHnvckBCe3OjeR?= M13iSVIh|ryP NV3t[pZ{PDhiaB?= MWDEUXNQ NWrt[Jo6[myxY3vzxsB1NUGXQ1KtbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKHSqZTDwN|ghVUGSSz;NRXBMSVCNMj;Id5AzPyCyYYToe4F6KGGwZDDpcohq[mm2czDlfJBz\XO|aX;uJI9nKE6LQ1Sx MlLRNlQ4QTN|MUO=
U87  NVz1RlB3TnWwY4Tpc44hSXO|YYm= M3TPSlIh|ryP NH3DWII1QCCq MY\EUXNQ M2O4NoJtd2Otc9MgeE1CXUOELXnu[JVk\WRiYXP0bZZifGmxbjDv[kB1cGVicEO4JG1CWEtxTVHQT2FRUzJxSIPwNlcheGG2aIfhfUBidmRiaX7obYJqfHNiZYjwdoV{e2mxbjDv[kBPUUOGMR?= NYf1WG1MOjR5OUOzNVM>
A549  MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDpNVAh|ryP MYmyOIg> M2rjfYRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkh[2:vYnnu[YQhf2m2aDDQWGU> MlP2NlM3PzF4MUm=
GC-B  M1:5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjROk4zPS1zMECg{txO NGr0ZXkzPCCq MYnEUXNQ NETqUHBqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MoHENVk2PDJ2NE[=

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アッセイ
Methods Test Index PMID
Western blot
Snail / N-cadherin / Vimentin / E-cadherin; 

PubMed: 24932308     


EMT markers were analyzed in AGS and MKN45 cells by immunoblotting following treatment with DAPT or the DMSO control.

Bax / caspase-3 / Bcl-2; 

PubMed: 29487808     


Western blot analysis of Bax, caspase-3, and Bcl-2 protein expression.

NICD / Pax7 / Pax3 / MyoD / Myogenin / p21; 

PubMed: 18957511     


(A) Primary myoblasts, incubated in GM until 90–100% confluency, were transferred to DM and were incubated for 1 day in the presence of DMSO or 5 μM GM6001, a metalloproteinase inhibitor (left), or in the presence of DMSO or 1 μM DAPT, a γ-secretase inhibitor (right). The levels of NICD, Pax7, Pax3, MyoD, myogenin, and p21 were determined by Western blotting, tubulin is a gel-loading control. A representative experiment out of three is shown.

24932308 29487808 18957511
Growth inhibition assay
Cell viability; 

PubMed: 27118928     


Cell viability of CPH036 or CPH047 cells following 7 days of treatment with iressa, DAPT or a combination in the indicated doses (mean ± SEM, n = 5). *p < 0.05, **p < 0.01, ***p < 0.001.

27118928
Immunofluorescence
CDK5; 

PubMed: 18662245     


Fixed E18 rat embryonic cortical neurons cells were immunostained for cdk5 (a, e) and p35 (b, f). Nuclei are stained with DAPI (c, g). Immunostaining for cdk5, p35 and DAPI are merged (d, h).

18662245
体内試験 DAPT administration (100mg/kg) leads to a robust and sustained pharmacodynamic effect in PDAPP mice that DAPT levels in the brain exceeds 100 ng/g within 1 hour and persists up to 18 hours after administration, with peak levels of 490 ng/g observed after 3 hour. And during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ and Aβ42 in a dose-dependent manner with a 50% reduction. [1] In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced activity of γ-secretase and increases the cell apoptosis with the prolonged neuroinflammation. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

In vitro Aβ reduction assays :

Human embryonic kidney cells (American Type Culture Collection CRL-1573), transfected with the gene for APP751 (HEK 293) are used for routine Aβ reduction assays. Cells are plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. DAPT are diluted from stock solutions in dimethylsulfoxide (DMSO) to yield a final concentration equal to 0.1% DMSO in media. Cells are pre-treated for 2 hours at 37 °C with DAPT, media are aspirated off and fresh compound solutions applied. After an additional 2-hour treatment period, conditioned media is drawn off and analyzed by a sandwich ELISA (266–3D6) specific for total Aβ. Reduction of Aβ production is measured relative to control cells treated with 0.1% DMSO and expressed as a percentage inhibition. Data from at least six doses in duplicate are fitted to a four-parameter logistical model using XLfit software in order to determine potency. Human and PDAPP mouse neuronal cultures are grown in serum-free media to enhance their neuronal characteristics, and appeared to be greater than 90% neurons after maturation prior to use. Conditioned media to establish baseline Aβ values are collected by adding fresh media to each well and incubated for 24 hours at 37 °C in the absence of DAPT. Cultures are then treated with fresh media containing DAPT at the desired range of concentrations for an additional 24 hours at 37 °C, and conditioned media collected. For the measurement of total Aβ, samples are analyzed with the same ELISA (266–3D6) as used for the HEK 293 cell assays. Analyses of samples for Aβ42 production are performed by a separate ELISA (21F12–3D6) that utilizes a capture antibody specific for the Aβ42 C-terminus. Inhibition of production for both total Aβ and Aβ42 are determined by the difference between the values for the compound treatment and baseline periods. After plotting percentage inhibition versus DAPT concentration, data are analyzed with XLfit software, as above, to determine potency.
細胞試験: [2]
- 合併
  • 細胞株: SK-MES-1
  • 濃度: 2.5 μM to 160 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cells are seeded into 96-well plates and exposed to 0.1% DMSO or DAPT at concentrations in the range of 2.5 μM–160 μM for 72 hours. Cytotoxicity is determined with 3-(4, 5)-dimethylthiahiazo-(-z-y1)-3, 5-di-phenytetrazoliumromide (MTT) dye reduction assay with minor modifications. Briefly, after incubation with DAPT, 20 μL MTT solution (5 mg/mL in PBS) is added to 180 μL medium in each well and plates are incubated for 4 hours at 37 °C, and subsequently 150 μL DMSO is added to each well, and mixed by shaking at room temperature for 15 minutes. Absorption is measured by an enzyme-linked immunosorbent assay at 490 nm to determine absorbance values. α-MEM supplemented with the same amount of MTT solution and solvent is used as blank solution. The IC50 value is calculated using PROBIT program in SPSS.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein.
  • 製剤: DAPT is dissolved in corn oil, 5% (v/v) ethanol.
  • 投薬量: ≤100 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

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 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 432.46
化学式

C23H26F2N2O4

CAS No. 208255-80-5
保管
in solvent
別名 LY-374973
Smiles CC(NC(=O)CC1=CC(=CC(=C1)F)F)C(=O)NC(C(=O)OC(C)(C)C)C2=CC=CC=C2

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03567733 Active not recruiting Device: XIENCE Sierra Ischemic Heart Disease|Coronary Artery Disease Fundación EPIC June 18 2018 --
NCT03190005 Unknown status Drug: clopidogrel|Drug: Placebos Stable Angina Taipei City Hospital January 1 2017 Not Applicable
NCT02548650 Completed Drug: Vorapaxar|Drug: Clopidogrel|Drug: Aspirin Myocardial Infarction|Diabetes Mellitus|Peripheral Arterial Disease University of Florida|Merck Sharp & Dohme Corp. March 25 2016 Phase 4
NCT03362463 Active not recruiting Other: Non-Interventional Study Acute Coronary Syndrom AstraZeneca December 28 2015 --
NCT03103620 Completed Device: COBRA PzF Coronary Stent System Stable Angina|Unstable Angina|ACS - Acute Coronary Syndrome|STEMI|NSTEMI - Non-ST Segment Elevation MI|Myocardial Infarction CeloNova BioSciences Inc.|AlpinARC September 10 2015 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

  • 質問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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID