GW4869

製品コード:S7609 別名:GW69A, GW554869A

For research use only.

GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor.

GW4869化学構造

CAS No. 6823-69-4

サイズ 価格(税別)
JPY 26400
JPY 84500

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(30)

質量管理及び製品安全説明書

Phospholipase (e.g. PLA)阻害剤の選択性比較

相関Phospholipase (e.g. PLA)製品

生物活性

製品説明 GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor.
ターゲット
SMase [1]
(Cell-free assay)
1 μM
体外試験

GW4869 inhibits N-SMase not only in vitro but also in a cellular model. GW4869 does not significantly impair TNF-induced NF-κB translocation to nuclei. Therefore, GW4869 does not interfere with other key TNF-mediated signaling effects. GW4869 is able, in a dose-dependent manner, to significantly protect from cell death as measured by nuclear condensation, caspase activation, PARP degradation, and trypan blue uptake. These protective effects are accompanied by significant inhibition of cytochrome c release from mitochondria and caspase 9 activation, therefore localizing N-SMase activation upstream of mitochondrial dysfunction. At up to 150 μM, GW4869 does not inhibit the cloned human A-SMase. GW4869 shows no or minor inhibitory activity versus other hydrolytic enzymes, such as bacterial phosphatidylcholine-PLC and bovine protein phosphatase 2A, and it shows significantly higher activity versus the rat brain enzyme compared with the human lyso-PAF PLC[1].

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 MVvGeY5kfGmxbjDhd5NigQ>? NHLnb|QyOC1{MDFOwG0> NH:0PVR1cGViYXTkbZRqd25ib3[gNVAh|ryPIFfXOFg3QSC|aXfubYZq[2GwdHz5JIlvcGmkaYTl[EBVVkZvaX7keYNm\CCVTTDofYRzd2y7c3nzMEB4cGW{ZXHzJFIxKM7:TTDv[kB1cGViY3;tdI92dmRicILveIVkfGWmIHPvcZBt\XSnbImg[pJwdSC2aHWgcI9{eyCxZjDzdIhqdmexbYnlcIlv NYPRcJN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxOVQxQThpPkGyNVU1ODl6PD;hQi=>
OPM2 MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 NGXjdlYxNCBzLkK1MEAzNjVuIEWsJFExNCB{MDygOFAh|ryvb3yvUC=> NUTpUllHOjRiaB?= M3PGRZRp\SClZXzsJJBzd2yrZnXyZZRqd25icnH0[UB4[XNiaX7jdoVie2WmIHHmeIVzKEeZNEi2PUB1emWjdH3lcpQvKFSqZTDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiC5YYOgc45tgSC|aXfubYZq[2GwdDD3bIVvKHSqZTDjc45k\W62cnH0bY9vKG:oIFfXOFg3QSC5YYOgOFAh|ryvb3yvUEBweiCqaXfo[ZIv NUnRb3ZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVgzQTRpPkK4PFU5Ojl2PD;hQi=>
RPMI-8226 M{fYOGNmdGxidnnhZoltcXS7IHHzd4F6 M3OwZVczKGh? NUTTOphQ[3m2b4TvfIlkKHSxIHGgdIFv\Wxib3[gUW0h[2WubDDsbY5mew>? Mo\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{MUG1O|MoRjJ6MkGxOVc{RC:jPh?=
NCI-H929 NGi1OnNE\WyuII\pZYJqdGm2eTDhd5NigQ>? NETBSJo4OiCq MnW2Z5l1d3SxeHnjJJRwKGFicHHu[Ywhd2ZiTV2gZ4VtdCCuaX7ldy=> NXW3R3l7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNVE2PzNpPkK4NlEyPTd|PD;hQi=>
JJN3 NH34cJFE\WyuII\pZYJqdGm2eTDhd5NigQ>? M1PjU|czKGh? NXG5NGFI[3m2b4TvfIlkKHSxIHGgdIFv\Wxib3[gUW0h[2WubDDsbY5mew>? NVLCOZZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNVE2PzNpPkK4NlEyPTd|PD;hQi=>
U266 NETQdmFE\WyuII\pZYJqdGm2eTDhd5NigQ>? MXu3NkBp NGDoWoVkgXSxdH;4bYMhfG9iYTDwZY5mdCCxZjDNUUBk\WyuIHzpcoV{ NH3SdmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKxNVU4Oyd-MkiyNVE2PzN:L3G+
Daudi NEXFUmdE\WyuII\pZYJqdGm2eTDhd5NigQ>? M1nT[lczKGh? M2nIOo5wfCCleYTveI95cWNidH:gco9vNU2PIHPlcIwhdGmwZYOgc5IhWEKPQ4O= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJzMUW3N{c,Ojh{MUG1O|M9N2F-
Jurkat NYHre5MzS2WubDD2bYFjcWyrdImgZZN{[Xl? Mni0O|IhcA>? NGrkUnpvd3RiY4n0c5RwgGmlIITvJI5wdi2PTTDj[YxtKGyrbnXzJI9zKFCETVPz NFfVNGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKxNVU4Oyd-MkiyNVE2PzN:L3G+
K562 MVjD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NHrJdlA4OiCq MX3uc5Qh[3m2b4TvfIlkKHSxIH7vck1OVSClZXzsJIxqdmW|IH;yJHBDVUO| MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJzMUW3N{c,Ojh{MUG1O|M9N2F-
PBMCs M2nmbmNmdGxidnnhZoltcXS7IHHzd4F6 M1uwc|czKGh? M4PBSo5wfCCleYTveI95cWNidH:gco9vNU2PIHPlcIwhdGmwZYOgc5IhWEKPQ4O= NIjmeFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKxNVU4Oyd-MkiyNVE2PzN:L3G+
アッセイ
Methods Test Index PMID
Immunofluorescence Nrf2 29794115
体内試験 Systemic administration of GW4869 does not alter the ceramide or sphingomylein content of liver, heart or skeletal muscle but does decrease the ceramide content and increase the sphingomyelin content in brain. Inhibition of nSMase2 with GW4869 slowed learning. Mice administered GW4869 do not progressively decrease latency to locate the hidden platform with repeated training trials, suggesting that they has difficulty learning to use spatial cues to navigate the pool[2]. Intraperitoneal injection of GW4869 reduces the levels of brain and serum exosomes, brain ceramide, and Aβ1-42 plaque load. GW4869 reduces amyloid plaque formation in vivo by preventing exosome secretion. GW4869 may have a low toxicity at levels needed to achieve a biological effect from nSMase2 inhibition[3].

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

  • 細胞株:MCF7 cells
  • 濃度: 10-20 μM
  • 反応時間:30 min
  • 実験の流れ:

    MCF7 human breast cancer cells are routinely cultured in RPMI 1640 containing 10% FBS at 37 °C in 5% CO2. Unless otherwise indicated, for treatment, cells are seeded at 1.7 × 106 cells/10-cm culture dish in 10 ml of complete medium; after 24 h, the medium is replaced with 7 ml of RPMI 1640 containing 2% FBS and 25 mM Hepes, pH 7.5, and the cells are rested for 2 h prior to treatment. GW4869 is routinely stored at −80 °C as a 1.5 mM stock suspension in Me2SO. Right before use, the suspension is solubilized by the addition of 5% methane sulfonic acid (MSA) (2.5 μl of 5% MSA in sterile double-distilled H2O are added to 50 μl of GW4869 stock suspension; therefore, the concentration of the GW4869 stock solution at the time of the experiments is 1.43 mM). The suspension is mixed and warmed up at 37 °C until clear. Cells are preincubated with the inhibitor for 30 min prior to treatment with TNF. Control cells are treated with Me2SO containing 5% MSA, similarly to the samples receiving the GW4869 solution. When different doses of GW4869 are tested, amounts of vehicle solution are added in order to equal the volume of GW4869 used for the highest dose.

動物試験:

[2]

  • 動物モデル:Mice with a complete loss of nSMase2 activity (background: C57BL/6J mice)
  • 投薬量:1.25 mg/kg
  • 投与方法:i.p.

溶解度 (25°C)

体外

化学情報

分子量 577.5
化学式

C30H28N6O2.2HCl.XH2O

CAS No. 6823-69-4
Storage 3年 -20°C
2年 -80°C in solvent
Smiles C1CN=C(N1)C2=CC=C(C=C2)NC(=O)C=CC3=CC=C(C=C3)C=CC(=O)NC4=CC=C(C=C4)C5=NCCN5.Cl.Cl

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

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

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: GW4869を買う | GW4869 ic50 | GW4869供給者 | GW4869を購入する | GW4869費用 | GW4869生産者 | オーダーGW4869 | GW4869化学構造 | GW4869分子量 | GW4869代理店