Cryptotanshinone (Tanshinone C)
中文名称：隐丹参酮
Cryptotanshinone (Tanshinone C)是一种STAT3抑制剂，无细胞试验中IC50为4.6 μM，强烈抑制STAT3 Tyr705磷酸化，对STAT3 Ser727作用效果弱，对STAT1和STAT5没有作用效果。Cryptotanshinone 可诱导ROS依赖的自噬和线粒体介导的凋亡。
Cryptotanshinone (Tanshinone C) Chemical Structure
CAS: 35825-57-1
产品质控
批次：
纯度：
99.75%
99.75
Cryptotanshinone (Tanshinone C)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Cryptotanshinone (Tanshinone C)是一种STAT3抑制剂，无细胞试验中IC50为4.6 μM，强烈抑制STAT3 Tyr705磷酸化，对STAT3 Ser727作用效果弱，对STAT1和STAT5没有作用效果。Cryptotanshinone 可诱导ROS依赖的自噬和线粒体介导的凋亡。 | ||
|---|---|---|---|
| 特性 | Cryptotanshinone 通过选择性抑制STAT3 活性，而具有抗肿瘤活性。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Cryptotanshinone是从Salvia miltiorrhiza Bunge(丹参)根中分离的天然化合物, 与丹参酮IIA（没有活性）相比，显著抑制STAT3依赖的荧光素酶活性, 且抑制STAT3 在Tyr705位点磷酸化，和STAT3的二聚体化。Cryptotanshinone (7 μM)处理 DU145细胞，在处理30分钟期间，显著抑制 STAT3 在Tyr705位点磷酸化，而不抑制STAT3在 Ser727位点磷酸化，且Cryptotanshinone(7 μM)处理4小时后，显著抑制JAK2 磷酸化，IC50为~5 μM，但是不影响下游激酶c-Src和 EGFR的磷酸化, 说明抑制STAT3 在Tyr705 位点磷酸化是因为与 STAT3的SH2域结合的直接机制。Cryptotanshinone显著抑制含组成型激活STAT3的DU145 前列腺癌细胞增殖，GI50 为7 μM，通过阻断 STAT3活性, 导致cyclin D1, Bcl-xL, 和 survivin的下调,随后导致在G0-G1期累积。Cryptotanshinone作用于PC3, LNCaP 和MDA-MB-468细胞，微弱抑制生长。[1] | |||
|---|---|---|---|---|
| 激酶实验 | STAT3依赖性双重荧光素酶实验 | |||
| 瞬时转染报告质粒的HCT-116 细胞具有 STAT3结合元件，用于调节荧光素酶检测。使用浓度为0.2 到50 μM的Cryptotanshinone处理细胞24小时。处理后，在20 μL裂解缓冲液中收集细胞，通过双重荧光素酶报告检测试剂盒在Wallac Victor2上测评荧光素酶活性。测定IC50值。 | ||||
| 细胞实验 | 细胞系 | KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa 和 HCT-116 | ||
| 浓度 | 溶于DMSO,终浓度为 ~50 μM | |||
| 孵育时间 | 24 或48小时 | |||
| 方法 | 使用 Cryptotanshinone处理细胞24或48小时。为了测定细胞增殖，加入细胞增殖试剂WST-1，使用ELISA 读数器在450 nm处定量分析WST-1 甲臜。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT3 / STAT3 / p-ERK / ERK |
|
30986607 | |
| Immunofluorescence | p-STAT3 / p-ERK |
|
30986607 | |
| Growth inhibition assay | Cell viability |
|
20820782 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Cryptotanshinone 处理ob/ob 小鼠(C57BL/6J-Lepob) 和饮食导致的肥胖 (DIO) 小鼠，显著降低体重和食物摄入，这种作用存在剂量依赖性。Cryptotanshinone处理脂肪组织，显著降低脂肪，显著降低血清甘油三酯和胆固醇水平，且 骨骼肌中, AMPK活性比对照组小鼠高2.5到 3倍。Cryptotanshinone每天按 600 mg/kg剂量处理ob/ob小鼠 (C57BL/6J-Lepob), db/db 小鼠(C57BL/KsJ-Leprdb), 和 ZDF 大鼠, 3天后，显著降低血糖水平，且在整个监测期都维持降低水平。[2] | |
|---|---|---|
| 动物实验 | Animal Models | Zucker糖尿病肥胖 (ZDF) (雄性) 2型糖尿病大鼠, ob/ob 小鼠(C57BL/6J-Lepob), db/db 小鼠 (C57BL/KsJ-Leprdb) 和高脂肪饮食引起肥胖的雄性C57BL/6J 小鼠 |
| Dosages | ~600 mg/kg/day | |
| Administration | 口服处理 | |
化学信息&溶解度
| 分子量 | 296.36 | 分子式 | C19H20O3 |
| CAS号 | 35825-57-1 | SDF | Download Cryptotanshinone (Tanshinone C) SDF |
| 储存条件(自收到货起) | |||
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体外溶解度 |
Ethanol : 10 mg/mL (33.74 mM) DMSO : 8 mg/mL ( (26.99 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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