Cryptotanshinone (Tanshinone C)

Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.

Cryptotanshinone (Tanshinone C)化学構造

CAS No. 35825-57-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 13600 国内在庫あり
JPY 13300 国内在庫あり
JPY 20500 国内在庫あり
JPY 36800 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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Cryptotanshinone (Tanshinone C)関連製品

シグナル伝達経路

STAT阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
U-973 Cell cycle assay 15 to 30 uM 24 hrs Cell cycle arrest at G1-S phase in PTPN11 G60R mutant harboring human U-973 cells at 15 to 30 uM after 24 hrs by FACS analysis 23957426
U-973 Apoptosis assay 15 to 30 uM 24 hrs Induction of apoptosis in PTPN11 G60R mutant harboring human U-973 cells at 15 to 30 uM after 24 hrs by FACS analysis 23957426
PTPN11 Function assay 1.5 to 6 uM 14 days Inhibition of GM-CSF-induced growth in PTPN11 E76K/+ myeloid progenitor cells from JMML patient at 1.5 to 6 uM after 14 days by inverted microscopic analysis 23957426
PTPN11 Function assay 1.5 to 6 uM 14 days Inhibition of GM-CSF-induced colony formation in PTPN11 E76K/+ myeloid progenitor cells from JMML patient at 1.5 to 6 uM after 14 days by inverted microscopic analysis 23957426
PTPN11 Function assay 1.5 to 15 uM 7 days Inhibition of GM-CSF-induced colony formation in PTPN11 E76K/+/Mxl-Cre+ mouse myeloid progenitor cells at 1.5 to 15 uM after 7 days by inverted microscopic analysis 23957426
Ba/F3 Function assay 30 uM 3 hrs Inhibition of IL3-induced SHP2-Gab2 interaction in mouse Ba/F3 cells pretreated at 30 uM for 3 hrs prior IL3 stimulation by immunoblotting method 23957426
AGS Function assay 24 hrs Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay, IC50=13.5μM 17583950
AGS Function assay 24 hrs Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay, IC50=10.2μM 17583950
AGS Function assay 16 hrs Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay, IC50=1.58μM 17583950
Hep3B Function assay 16 hrs Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay, IC50=1.36μM 17583950
KBV1 Cytotoxicity assay 48 hrs Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay, IC50=7.5μM 11720520
KB-3-1 Cytotoxicity assay 48 hrs Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay, IC50=6.9μM 11720520
MIAPaCa2 Cytotoxicity assay 24 hrs Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay, IC50=5.8μM 21775156
HCT116 Function assay 24 hrs Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay, IC50=4.6μM 22650325
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay, IC50=17.22μM 23957426
HeLa Growth inhibition assay 24 hrs Growth inhibition of human HeLa cells after 24 hrs 23957426
THLE3 Cytotoxicity assay Cytotoxicity against human THLE3 cells by MTT assay, EC50=22.9μM 20455578
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells by MTT assay, CD50=29.7μM 16038550
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells by MTT assay, CD50=17.2μM 16038550
OVCAR-3 Cytotoxicity assay Cytotoxicity against human OVCAR-3 cells by MTT assay, CD50=9.12μM 16038550
HepG2 Apoptosis assay Induction of apoptosis in human HepG2 cells expressing wild type p53 gene assessed as caspase 3 activation 20455578
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
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生物活性

製品説明 Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Targets
STAT3 [1]
(HCT-116 cells)
4.6 μM
In Vitro
In vitro Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705 phosphorylation and the dimerization of STAT3, compared to tanshinone IIA which exhibits no activity. Cryptotanshinone (7 μM) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of ~5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR, suggesting the inhibition of STAT3 Tyr705 phosphorylation might due to a direct mechanism probably by binding to the SH2 domain of STAT3. Cryptotanshinone significantly inhibits the proliferation of DU145 prostate cancer cells harboring constitutively active STAT3 with GI50 of 7 μM by blocking STAT3 activity, which leads to the down-regulation of cyclin D1, Bcl-xL, and survivin, subsequently the accumulation in the G0-G1 phase. Cryptotanshinone exhibits less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells. [1]
Kinase Assay STAT3-dependent dual-luciferase assay
HCT-116 cells are transiently transfected with reporter plasmid having the STAT3-binding element for regulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of 0.2 to 50 μM. After treatment, cells are harvested in 20 μL of passive lysis buffer and luciferase activity is evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of Cryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.
細胞実験 細胞株 KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116
濃度 Dissolved in DMSO, final concentrations ~50 μM
反応時間 24 or 48 hours
実験の流れ Cells are exposed to Cryptotanshinone for 24 or 48 hours. For the determination of cell proliferation, the cell proliferation reagent WST-1 is added and WST-1 formazan is quantitatively measured at 450 nm using an ELISA reader.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-STAT3 / STAT3 / p-ERK / ERK 30986607
Immunofluorescence p-STAT3 / p-ERK 30986607
Growth inhibition assay Cell viability 20820782
In Vivo
In Vivo Cryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period. [2]
動物実験 動物モデル Zucker Diabetic Fatty (ZDF) (male) type 2 diabetic rat, ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb) and male C57BL/6J mice with high-fat diet-induced obesity
投与量 ~600 mg/kg/day
投与経路 Orally

化学情報

分子量 296.36 化学式

C19H20O3

CAS No. 35825-57-1 SDF Download Cryptotanshinone (Tanshinone C) SDFをダウンロードする
保管

In vitro
Batch:

Ethanol : 10 mg/mL

DMSO : 8 mg/mL ( (26.99 mM); Warmed with 50℃ water bath; 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

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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よくある質問(FAQ)

質問1:
I want to use this compound for my mouse in vivo experiment, so how to reconstitute it?

回答
Cryptotanshinone can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 2 mg/ml. But after stayed for about 0.5-1 hour, the precipitation went out. So if you are going to use this vehicle, it is recommended to be prepared just before use.

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