CAY10585 (LW 6)

別名:AC1-001

CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays.

CAY10585 (LW 6)化学構造

CAS No. 934593-90-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫なし(納期7~10日)
JPY 115500 国内在庫あり
JPY 448500 国内在庫なし(納期7~10日)

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(13)

製品安全説明書

現在のバッチを見る: 純度: 99.12%
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CAY10585 (LW 6)関連製品

シグナル伝達経路

HIF阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HeLa Function assay 30 uM 4 hrs Inhibition of hypoxia-induced HIF1alpha nuclear translocation in human HeLa cells at 30 uM after 4 hrs by immunofluorescence analysis 24900662
HeLa Function assay 30 uM 4 hrs Inhibition of hypoxia-induced HIF1alpha accumulation in human HeLa cells at 30 uM after 4 hrs by Western blot analysis 24900662
HCCLM3 Function assay 10 uM 1 hr Inhibition of HIF1alpha accumulation in hypoxia-induced human HCCLM3 cells at 10 uM incubated with compound under normoxia for 1 hr followed by hypoxia induction and measured after 24 hrs by Western blot analysis 31556611
Hep3B Function assay 10 uM Suppression of hypoxia-induced VEGF mRNA expression in human Hep3B cells at 10 uM 17328532
Hep3B Function assay 10 uM Suppression of hypoxia-induced EPO mRNA expression in human Hep3B cells at 10 uM 17328532
HCT116 Function assay 10 uM Reduction in ATP production in human HCT116 cells at 10 uM by luciferase based assay 25356789
HCT116 Function assay 10 uM Inhibition of MDH2 in human HCT116 cells assessed as AMPK activation at 10 uM by immunoblot assay 25356789
HCT116 Function assay 10 uM Inhibition of MDH2 in human HCT116 cells assessed as reduction in ACC phosphorylation at 10 uM by immunoblot assay 25356789
HCT116 Function assay 16 hrs Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay, IC50=2.44μM 23153200
HeLa Function assay 12 hrs Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay, IC50=21μM 24900662
HCT116 Function assay 12 hrs Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay, IC50=4.4μM 25356789
AGS Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50=0.7μM 17328532
Hep3B Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay, IC50=2.6μM 17328532
HCCLM3 Function assay Inhibition of HIF1alpha transcriptional activity in hypoxia-induced human HCCLM3 cells co-transfected with luciferase reporter plasmid containing five copies of HREs and pRL-SV40 plasmid encoding Renilla luciferase incubated with compound under normoxia f, IC50=3.08μM 31556611
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生物活性

製品説明 CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays.
Targets
BCRP [3] HIF [2]
(Cell-free assay)
MDH2 [2]
(Cell-free assay)
4.4 μM 6.3 μM
In Vitro
In vitro

LW6 inhibits HIF-1α expression induced by hypoxia. It promotes apoptosis preferentially in hypoxic cells. Treatment with LW6 presents no additive effect on cell cycle arrest. LW6 induces ROS formation through the depolarization of MMP in hypoxic cells. Although LW6 increases mitochondrial ROS production, the combination with hypoxia induces a marked increase in ROS production and this high level is maintained up until 24 h. LW6 is also a specific inhibitor of MDH2. As MDH2 is known to serve a significant role in the citric acid cycle at the mitochondrial membrane, LW6 indirectly reduces the activity of the mitochondrial respiratory chain through the inhibition of MDH2[1].In contrast to BCRP, LW6 has no inhibition effect on the functional activity and gene expression of P-gp[2]. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM. Furthermore, cells become more susceptible to the cytotoxicity of anticancer drugs in the presence of LW6[3].

細胞実験 細胞株 A549 cells
濃度 5-100 μM
反応時間 24 h
実験の流れ

Cells are incubated in 96-well ELISA Plates with 100 μl culture medium at 2×105 cells/ml with or without LW6 for 24 h. Cell viability is assessed by the dimethyl thiazolcarboxy-methoxyphenylsulfophenyltetrazolium (MTS) assay. The absorbance is measured at 490 and 620 nm using a microplate reader. For the trypan blue dye. exclusion test, cells are stained by phosphate-buffered saline (PBS) containing 0.1% trypan blue. Cell viability is assessed by counting the number of unstained cells.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot HIF-1α E-cadherin / PIMT 26017562
In Vivo
In Vivo

LW6 exerts marked anti-tumor efficacy in vivo and causes reductions in HIF-1α expression levels in mice carrying xeno-grafts of HCT116 cells[1]. LW6 improves the cytotoxicity and bioavailability of anticancer drugs translocated by BCRP[3].

動物実験 動物モデル Male Sprague-Dawley rats
投与量 10 mg/kg
投与経路 p.o.

化学情報

分子量 435.51 化学式

C26H29NO5

CAS No. 934593-90-5 SDF Download CAY10585 (LW 6) SDFをダウンロードする
Smiles COC(=O)C1=CC(=C(C=C1)O)NC(=O)COC2=CC=C(C=C2)C34CC5CC(C3)CC(C5)C4
保管

In vitro
Batch:

DMSO : 24 mg/mL ( (55.1 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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