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Sirtinol

Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.

Sirtinol化学構造

CAS No. 410536-97-9

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（44）

質量管理及び製品安全説明書

S280401 DMSO] 23 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度：>97%
97

Sirtinol関連製品

シグナル伝達経路

Sirtuin Signaling Pathways

Sirtuinシグナル伝達経路

Sirtuin阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human MCF7 cells Function assay 50 μM 24 h Inhibition of SIRT1 in human MCF7 cells assessed as increase in acetylation of p53 at lys 382 at 50 uM after 24 hrs by Western blot analysis 24340169
human MCF7 cells Proliferation assay 30 μM 24-72 h Antiproliferative activity against human MCF7 cells at 30 uM after 24 to 72 hrs 24340169
human U937 cells Apoptosis assay 50 μM 45 h Induction of apoptosis in human U937 cells at 50 uM after 45 hrs by flow cytometry 23189967
Hs683 Antiproliferative assay 72 hrs Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay, IC50=33.9μM 28475330
U373 Antiproliferative assay 72 hrs Antiproliferative activity against human U373 cells after 72 hrs by MTT assay, IC50=39.3μM 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at G1 phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
U373 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human U373 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
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生物活性

製品説明 Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
特性 Sirtinol does not inhibit class I and class II HDACs.
Targets
SIRT2 [1]
(Cell-free assay)		 SIRT1 [2]
(Cell-free assay)
38 μM 131 μM
In Vitro
In vitro Sirtinol potently inhibits recombinant yeast Sir2p activity in vitro with IC50 of 68 μM. Unlike TSA, Sirtinol has shown no effect on human HDAC1, indicating that it is a selective sirtuin inhibitor. Unlike TSA, treatment of human primary fibroblasts with Sirtinol does not cause global changes in acetylation of histones and tubulin, nor does it induce a morphological change in the HeLa tumor cell line. [1] Sirtinol treatment at 100 μM for 24 hours causes a sustained growth arrest in MCF-7 and H1299 cells for up to 9 days after Sirtinol withdrawal. Sirtinol treatment induces increased SA-β-gal activity and expression of PAI-1 in both MCF-7 and H1299 cells, more potently than Splitomicin. Sirtinol inhibits colony formation at concentrations of 33 μM and higher in MCF-7 and H1299 cells, more effectively compared with Splitomicin. Sirtinol treatment (100 μM) significantly attenuates both basal and EGF- or IGF-I-stimulated phosphorylation of ERK, JNK/SAPK and p38 MAPK in MCF-7 and H1299 cells. Sirtinol blocks the basal and EGF-stimulated activation of Ras. Consistent, basal and EGF- or IGF-I-stimulated phosphorylation of Raf-1, MEK, SEK1/MKK4 and MKK7 is attenuated in Sirtinol-treated cells. [3] Inhibition of Sirt1 by Sirtinol enhances UV- and H2O2-induced p53 acetylation to enhance cell death in cultured skin keratinocytes. [6] Blocking of Sirt1 by Sirtinol treatment results in a significant inhibition in the growth and viability of human PCa cells while having no effect on normal prostate epithelial cells. [7]
Kinase Assay Inhibition in vitro of human Sirt2 activity
1.5 μg of recombinant human GST-Sirt2 (amino acids 18-340) are incubated at 30°C for 2 hours in 50 μL of assay buffer (50 mM Tris-HCl, pH 8.8, 4 mM MgCl2, 0.2 mM dithiothreitol with different concentrations of Sirtinol, 50 μM NAD, and tritiated acetylated HeLa histones (1000 cpm), purified by acid extraction. HDAC activity is determined by scintillation counting of the ethyl acetate-soluble [3H]acetic acid.
細胞実験 細胞株 LNCaP, 22Rv1, DU145, and PC3
濃度 Dissolved in DMSO, final concentrations ~120 μM
反応時間 24 or 48 hours
実験の流れ

Cells are grown to 60% confluence and then treated with 30 μM or 120 μM sirtinol for 24 or 48 hours. Cells are trypsinized and collected. The cells are pelleted by centrifugation and resuspended in PBS (120 μL). Trypan blue (0.4% in PBS; 10 μL) is added to a smaller aliquot (10 μL) of cell suspension, and the number of cells (viable unstained and nonviable blue) are counted.
実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay Cell viability 25184156
Western blot SIRT1 / p-AKT / Foxo3a / β-catenin Foxp3 / RORγt Ac-H3K9 / Fibrobectin / Collagen 1 / α-SMA 25184156
In Vivo
In Vivo Administration of Sirtinol at 1 mg/kg attenuates pro-inflammatory cytokine production and protects against hepatic injury following trauma-hemorrhage in male Sprague-Dawley rats. [4]
動物実験 動物モデル Male Sprague-Dawley rats subjected to trauma-hemorrhage
投与量 1 mg/kg
投与経路 Administered intravenously

化学情報

分子量 394.47 化学式

C26H22N2O2
CAS No. 410536-97-9 SDF Download Sirtinol SDFをダウンロードする
Smiles CC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2N=CC3=C(C=CC4=CC=CC=C43)O
保管

In vitro
Batch:

DMSO : 23 mg/mL ( (58.3 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 匹

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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