VPS34 inhibitor 1 (Compound 19)

別名:PIK-III analogue

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

VPS34 inhibitor 1 (Compound 19)化学構造

CAS No. 1383716-46-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 52300 国内在庫なし(納期7~10日)
JPY 26400 国内在庫あり
JPY 46800 国内在庫あり
JPY 146400 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(8)

カスタマーフィードバック1个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.27%
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VPS34 inhibitor 1 (Compound 19)関連製品

シグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NCOA4 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of p62 degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NBR1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NDP52 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of FTH1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as increase in LC3-1 protein expression at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as increase in LC3-2 protein expression at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
U2OS Function assay 2 hrs Inhibition of VPS34 in human U2OS cells incubated for 2 hrs by GFP-FYVE reporter gene assay, IC50=0.025μM 26819669
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生物活性

製品説明 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
Targets
VPS34 [1]
(Cell-free assay)
15 nM
In Vitro
In vitro Compound 19 is extraordinarily selective over other lipid and protein kinases. The ability of compound 19 to prevent the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1 is similar to PIK-III. In addition, treatment of cells with compound 19 leads to an increase in the lipidated and nonlipidated forms of LC3 similar to previous reports using PIK-III[1].
細胞実験 細胞株 U2OS cells
濃度 0, 1, 5, 10 μM
反応時間 24 h
実験の流れ For inhibitor assay, cells are plated and the following day when cells had reached 90%, are treated with dimethyl sulfoxide (DMSO, vehicle) or the indicated concentration of PIK-III or Compound 19, both dissolved in DMSO. 24 hours later, cells are lysed in RIPA supplemented with 1% SDS and mini-EDTA protease inhibitors, homogenized by passage through a Qiashredder column and the protein is quantified by DC Lowry protein assay.
In Vivo
In Vivo The pharmacokinetic profile of analogue 19 is determined in C57BL/6 mice. After oral administration at 10 mg/kg, the compound is rapidly absorbed and showed moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47). Based on these PK parameters and the cellular activity, compound 19 constitutes a suitable candidate for in vivo studies. Upon oral administration of compound 19 at 50 mg/kg twice a day (BID) for 7 days, LC3-II accumulates consistent with reduced autophagic capacity in time-dependent manner. It inhibits autophagy in vivo[1].
動物実験 動物モデル C57BL/6 Mice
投与量 10 mg/kg(p.o.) or 2 mg/kg(I.V.)
投与経路 oral administration or I.V.

化学情報

分子量 391.47 化学式

C21H25N7O

CAS No. 1383716-46-8 SDF Download VPS34 inhibitor 1 (Compound 19) SDFをダウンロードする
Smiles CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC=NC=C4)O
保管

In vitro
Batch:

DMSO : 78 mg/mL ( (199.24 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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。

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Handling Instructions

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