Cryptotanshinone |
| Catalog No.GN10501 |
Cryptotanshinone is a natural compound extracted from the roots of Salvia miltiorrhiza Bunge, exhibiting antitumor activity by inhibiting Signal Transducer and Activator of Transcription 3 (STAT3) with an IC50 value of 4.6μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 35825-57-1
Sample solution is provided at 25 µL, 10mM.
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Cryptotanshinone is a natural compound extracted from the roots of Salvia miltiorrhiza Bunge, exhibiting antitumor activity by inhibiting Signal Transducer and Activator of Transcription 3 (STAT3) with an IC50 value of 4.6μM[1, 2]. Cryptotanshinone possesses multiple biological activities, including antitumor, anti-inflammatory, anti-fibrotic, and anti-angiogenic effects[3, 4].
In vitro, Cryptotanshinone (20μM) treatment of A549 cells for 24h reduced the percentage of cells in the G0/G1 phase, increased the percentage of cells in the G2/M phase, induced G2/M phase arrest, and promoted apoptosis along with the expression of apoptotic genes[5]. In another study, pretreatment of H9C2 cells with Cryptotanshinone (3μM) for 1h significantly prevented chronic hypoxia-induced cell injury, restored cellular ATP levels, reduced mitochondrial superoxide levels, and decreased intracellular NO and calcium levels[6].
In vivo, Cryptotanshinone (50mg/kg/day) administered via gastric gavage for 4 weeks in a mouse model of cardiac remodeling induced by aortic banding (AB) surgery improved pressure overload-induced cardiac dysfunction, attenuated cardiac hypertrophy, and reduced cardiac fibrosis[7]. Additionally, Cryptotanshinone (40mg/kg/day) administered orally in a CCl4-induced liver fibrosis mouse model ameliorated liver fibrosis, inhibited the activation of hepatic stellate cells, and suppressed collagen production[8].
References:
[1] Zheng J, Zhou Y, Zhang P, et al. Salvia miltiorrhiza Bunge: Bioactive Compounds and Bioactivities[J]. Int. J. Trad. Nat. Med, 2015, 5(1): 52-81.
[2] Hua Y, Yuan X, Shen Y, et al. Novel STAT3 inhibitors targeting STAT3 dimerization by binding to the STAT3 SH2 domain[J]. Frontiers in Pharmacology, 2022, 13: 836724.
[3] Li H, Gao C, Liu C, et al. A review of the biological activity and pharmacology of cryptotanshinone, an important active constituent in Danshen[J]. Biomedicine & Pharmacotherapy, 2021, 137: 111332.
[4] Hur J M, Shim J S, Jung H J, et al. Cryptotanshinone but not tanshinone IIA inhibits angiogenesis in vitro[J]. Experimental & molecular medicine, 2005, 37(2): 133-137.
[5] Chen L, Wang H J, Xie W, et al. Cryptotanshinone inhibits lung tumorigenesis and induces apoptosis in cancer cells in vitro and in vivo[J]. Molecular medicine reports, 2014, 9(6): 2447-2452.
[6] Jin H J, Li C G. Tanshinone IIA and cryptotanshinone prevent mitochondrial dysfunction in hypoxia‐induced H9c2 cells: association to mitochondrial ROS, intracellular nitric oxide, and calcium levels[J]. Evidence‐Based Complementary and Alternative Medicine, 2013, 2013(1): 610694.
[7] Li W, Yan H, Zhou Z, et al. Cryptotanshinone attenuated pathological cardiac remodeling in vivo and in vitro experiments[J]. Oxidative Medicine and Cellular Longevity, 2023, 2023(1): 4015199.
[8] Li Z, Zheng Y, Zhang L, et al. Cryptotanshinone alleviates liver fibrosis via inhibiting STAT3/CPT1A-dependent fatty acid oxidation in hepatic stellate cells[J]. Chemico-Biological Interactions, 2024, 399: 111119.
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were seeded in a 6-well plate at a density of 1x105/ml and treated at a final Cryptotanshinone concen tration of 20µM for 24h. Cells were trypsinized, centrifuged (4˚C, 800g/min, 10min), washed with PBS and fixed with cold 70% ethanol/30% PBS at 4˚C overnight. Cells were digested by RNase A, and then stained with 1% propidium iodide at 37˚C for 30min. The DNA profiles were determined within 4h of staining by flow cytometry. The expresions of cell cycle and apoptosis-associated genes was tested using Cell Cycle PCR Array. |
Reaction Conditions | 20μM; 24h |
Applications | Following treatment with 20µM Cryptotanshinone, the percentage of A549 cells in G0/G1 phase was decreased while that in G2/M phases was increased. Cryptotanshinone was able to cause G2/M phase arrest in A549 cells. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | After Aortic Banding (AB) surgery, the mice were divided into four groups randomly: saline group (VEH), Cryptotanshinone (CTS) group, AB group, and AB+CTS group (n=10 in the sham group, n=10 in the AB group). Three days after AB surgery, mice were administrated with Cryptotanshinone for 4 weeks (50mg/kg, gastric perfusion). At the end of the treatment, the surviving mice were used for accessing cardiac function. And mice were euthanized with an overdose of sodium pentobarbital (200mg/kg, intraperitoneal injection). Hearts were collected for other experiments. |
Dosage form | 50mg/kg; 4 weeks; gastric perfusion |
Applications | Cryptotanshinone treatment improved pressure overload-induced cardiac dysfunction, attenuated cardiac hypertrophy, and reduced cardiac fibrosis in mice. |
References: | |
| Cas No. | 35825-57-1 | SDF | |
| Chemical Name | (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 | ||
| Formula | C19H20O3 | M.Wt | 296.35 |
| Solubility | ≥ 4.23mg/mL in DMSO | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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