DAPT (GSI-IX)

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)  
JPY 18592.00
JPY 11620.00
JPY 19920.00
JPY 34860.00
JPY 61420.00

カスタマーフィードバック(9)

  • 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.

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− Mnq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqyJO69VQ>? Mn3yOFghcA>? M2fUfYVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7keYNm\CCkeTDDSGRR Mmi4NlQ2ODJ7NEm=
A549 CD133+ NIfwdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqyJO69VQ>? NHexNnA1QCCq M1rs[oVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7keYNm\CCkeTDDSGRR MWOyOFUxOjl2OR?=
HT29  MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTSdGJTOC53LUe1JO69VQ>? NInDbnAyOi9{ND:0PEBp MXXEUXNQ Ml7WbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh[2:wY3XueJJifGmxbjDtZY5v\XJ? MoDJNlUzPTd7NEW=
SHG-44 NVrtbId[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\ENE42NTFyIN88US=> NIDM[|QyNTViZB?= NHvGRphqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkh[XRidHjlJI9xfGmvYXygZ49v[2WwdILheIlwdiCxZjCxJO69VQ>? M{HPWFI2ODZ|Mki1
MG63 MlTRSpVv[3Srb36gRZN{[Xl? M{P4OFExOCEQvF2= NYDYWmdxOjRiaB?= MXvEUXNQ NHjEZoNl\XOnboPpeIl7\XNidHjlJINmdGxibHnu[UB1dyClaYPwcIF1cW5idILlZZRu\W62 NF7kO4IzPDh7NEK5Oy=>
Saos-2 MmLwSpVv[3Srb36gRZN{[Xl? MWKxNFAh|ryP M3L1N|I1KGh? NEnzVoNFVVOR NHzuNFdl\XOnboPpeIl7\XNidHjlJINmdGxibHnu[UB1dyClaYPwcIF1cW5idILlZZRu\W62 NHnGXYUzPDh7NEK5Oy=>
U251 Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHHNkDPxE1? MkLSOFghcA>? NXu4e5hHTE2VTx?= NUewU2Z3e3S{ZX7neIhmdnQEoIStRXVESi2rbnT1Z4VlKGOnbHyg[5Jwf3SqIIP1dJBz\XO|aX;u MY[yOFc6OzNzMx?=
U87  NESw[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUO5fo5LOiEQvF2= MljqOFghcA>? NWD2SXp[TE2VTx?= Mnz5d5Rz\W6pdHjlcpPDqHRvQWXDRk1qdmS3Y3XkJINmdGxiZ4Lve5RpKHO3cIDy[ZN{cW:w M1vrVlI1Pzl|M{Gz
U251 MoLxSpVv[3Srb36gRZN{[Xl? M{LROFIh|ryP NYj5PGRjPDhiaB?= NY\F[JBQTE2VTx?= MX\icI9kc3QEoIStRXVESi2rbnT1Z4VlKGGldHn2ZZRqd25ib3[geIhmKHB|ODDNRXBMN02DUFvBVGszN0i|cEK3JJBifGi5YYmgZY5lKGmwaHnibZR{KGW6cILld5Nqd25ib3[gUmlETDF? M2DlfFI1Pzl|M{Gz
U87  NX;We2ROTnWwY4Tpc44hSXO|YYm= MU[yJO69VQ>? M3rrXlQ5KGh? NVPjbYZMTE2VTx?= NGXGPWpjdG:la4RCpJQuSVWFQj3pcoR2[2WmIHHjeIl3[XSrb36gc4YhfGinIICzPEBOSVCNL13BVGtCWEt{L1jzdFI4KHCjdHj3ZZkh[W6mIHnubIljcXS|IHX4dJJme3Orb36gc4YhVkmFREG= NVrDbohJOjR5OUOzNVM>
A549  M4W4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHwZ3kyOCEQvF2= MofuNlRp MknQ[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkd22kaX7l[EB4cXSqIGDUSS=> Mn;XNlM3PzF4MUm=
GC-B  NF7MWWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYm2MlI2NTFyMDFOwG0> MVKyOEBp M4rneWROW09? Mnf0bY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NGHNNIwyQTV2MkS0Oi=>

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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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 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

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 (g) = 濃度 (mol/L) x 体積 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03355742 Recruiting Bleeding Disorder|Stroke Ischemic|Stroke Hemorrhagic|Hematological Disease|Thrombocytopenia|Coagulation Disorder|Anemia|Renal Insufficiency|Coronary Artery Disease Abbott Vascular February 9 2018 Not Applicable
NCT03606642 Not yet recruiting Coronary Artery Disease|Atherosclerosis|Stent Placement HonorHealth Research Institute|Boston Scientific Corporation July 23 2018 Phase 2
NCT03647475 Not yet recruiting Coronary Artery Disease Medtronic Vascular October 2018 Not Applicable
NCT03008083 Not yet recruiting Drug-Eluting Stents|Percutaneous Coronary Intervention Shanghai MicroPort Medical (Group) Co. Ltd. August 2018 Phase 4
NCT02798913 Unknown status Peripheral Artery Disease Federico II University January 2016 Phase 3
NCT02619760 Active not recruiting Coronary Artery Disease Kyoto University Graduate School of Medicine December 2015 Phase 4

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/

Gamma-secretaseシグナル伝達経路

Gamma-secretase Inhibitors with Unique Features

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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