Cryptotanshinone
(Synonyms: 隐丹参酮; Cryptotanshinon; Tanshinone c) 目录号 : GN10501
A natural quinoid diterpene with diverse actions
Cas No.:35825-57-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Kinase experiment: |
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. |
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Cell experiment: |
The MTT assay is used for the assessment of cell growth inhibition as described previously. Cells are seeded at a density of 8000 cells per well in 96-well plates in RPMI-1640 containing 10% FBS. Different concentrations of imatinib and CPT are added and incubated for another 24 h. Then, 20 μL of MTT are added into each well and the absorbance at 570 nm is measured on an enzyme linked immunosorbent assay (ELISA) plate reader. The coefficient of drug interaction (CDI) between imatinib and CPT is determined according to a previous study. The calculated method is as follows: CDI/AB/(A × B). According to the absorbance of each group, AB is the ratio of the combination group to the control group; A or B is the ratio of the single agent group to the control group. CDI 1 indicates an antagonistic effect. In the combination treatment group, the concentrations of CPT are arbitrarily designated according to the 50% inhibitory concentration (IC50) value. Then, the cell viabilities are determined after treatment with different concentrations of imatinib plus CPT (constant CPT concentration for one cell type). Finally, the combination IC50 values of imatinib are calculated, and are represented in Table I. The primary CML cells CP1 to CP3 are isolated from patients in chronic phase, while BC1 and BC2 are isolated from patients in blast crisis. Three independent sets of experiments are performed. The IC50 values are presented as the mean±standard deviation (SD). |
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References: [1]. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202. |
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Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
Cryptotanshinone 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 appr 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]. Cryptotanshinone significantly attenuates the in vitro hormonal effects of DEX on ovaries, as indicated by a significant decrease in T and an increase in P levels in the culture medium. Cryptotanshinone significantly increases the levels of phosphorylated AKT2 and GSK3β in the DEX-treated ovaries[2]. Cotreatment with imatinib and Cryptotanshinone shows a significant synergistic killing effect in both imatinib sensitive and resistant CML cell lines, as well as primary CML cells[3].
Cryptotanshinone reverses the ovarian IR and significantly increases 2-deoxy-D-[1,2-3H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rate and plasma E2 and P levels[2]. 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[4].
References:
[1]. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202.
[2]. Huang Y, et al. Cryptotanshinone reverses ovarian insulin resistance in mice through activation of insulin signaling and the regulation of glucose transporters and hormone synthesizing enzymes. Fertil Steril. 2014 Aug;102(2):589-596.e4.
[3]. Ge Y, et al. Cryptotanshinone acts synergistically with imatinib to induce apoptosis of human chronic myeloid leukemia cells. Leuk Lymphoma. 2014 Jun 25:1-9.
[4]. Kim EJ, et al. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase. Mol Pharmacol. 2007 Jul;72(1):62-72. Epub 2007 Apr 11.
| Cas No. | 35825-57-1 | SDF | |
| 别名 | 隐丹参酮; Cryptotanshinon; Tanshinone c | ||
| 化学名 | (1R)-1,6,6-trimethyl-2,7,8,9-tetrahydro-1H-naphtho[1,2-g][1]benzofuran-10,11-dione | ||
| Canonical SMILES | CC1COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCCC4(C)C | ||
| 分子式 | C19H20O3 | 分子量 | 296.35 |
| 溶解度 | ≥ 4.23mg/mL in DMSO | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3744 mL | 16.8719 mL | 33.7439 mL |
| 5 mM | 0.6749 mL | 3.3744 mL | 6.7488 mL |
| 10 mM | 0.3374 mL | 1.6872 mL | 3.3744 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。