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Thiostrepton,Also known as NSC 170365, FOXM1 Inhibitor I,Protein synthesis inhibitor,Bryamycin,NSC 81722,Thiactin,Thiostreptin A, It is a compound with specific biological activity The appearance is a white to off white solid with a solubility of ≥ 10mg/mL in DMSO and 25mg/mL in DMF, insoluble in water. It has a solubility of approximately 0.5mg/ml in a 1:1 solution of DMF and PBS (pH 7.2). The purity is generally higher than 95%. It is a natural cyclic oligopeptide antibiotic and a natural product of ribosomal synthesis and post-translational modified peptides (RIPPs). It exhibits antibiotic activity by prolonging the steps in protein synthesis, blocking the dissociation of elongation factor G (EF-G) in ribosomes, and releasing inorganic phosphates from EF-G after GTP hydrolysis. At the same time, it is also an inhibitor of FOXM1, which can inhibit FoxM1 in mammalian cells, prevent the expression of genes regulated by FoxM1 (including FoxM1 itself), thereby preventing human cancer cell proliferation and inducing cell apoptosis. This compound has a wide range of applications in molecular biology, pharmacology, and other scientific research fields, and can be used as a research reagent. It can only be used for scientific research experiments and is strictly prohibited for clinical medical and other purposes. Its storage conditions are -20 ℃, away from light, moisture-proof, sealed and dry. After dissolving in the solvent, please try to use it within one month at -20 ℃.
Additional information of chemical compound:
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Chemical Formula |
C72H85N19O18S5 |
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Exact Mass |
1663.49 |
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Molecular Weight |
1664.89 |
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m/z |
1663.49(100.0%),1664.50(77.9%),1665.50(29.9%),1665.49(22.6%),1666.49(17.6%),1666.50(7.5%),1667.49(6.8%),1664.49(6.6%),1665.49(5.5%),1664.49(4.0%),1665.50(3.7%),1665.50(3.1%),1666.50(2.9%),1667.48(2.0%),1666.50(2.0%),1668.50(1.7%),1668.49(1.6%),1666.49(1.5%),1667.49(1.2%),1666.50 (1.2%),1667.50(1.1%),1667.51 (1.1%) |
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Elemental Analysis |
C, 51.94; H, 5.15; N, 15.99; O, 17.30; S, 9.63 |
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Melting point |
248-257℃(dec.) |
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Density |
1.0824 (rough estimate) |
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Storage condition |
under -20℃ |
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Thiostrepton is mainly used in scientific research, especially as an important antibiotic and protein synthesis inhibitor, playing a key role in molecular biology, pharmacology and other research. The following is a detailed explanation of its purpose:
Inhibit protein synthesis: One of its main biological activities is to exert antibiotic effects by inhibiting protein synthesis. During protein synthesis, this substance can block the dissociation of elongation factor G (EF-G) in ribosomes and the release of inorganic phosphate from EF-G after GTP hydrolysis, thereby interfering with the normal progress of protein synthesis. This inhibitory effect makes it an effective antibiotic that can combat a variety of microorganisms.
Inhibition of cancer cell proliferation: In addition to being used as an antibiotic, it has also been found to have the ability to inhibit cancer cell proliferation. It achieves this by inhibiting the activity of the Forkhead box M1 (FOXM1) transcription factor. FOXM1 is overexpressed in many malignant tumors and is involved in regulating key biological processes such as cell cycle, DNA damage repair, and angiogenesis. It can selectively inhibit the activity of FOXM1, thereby preventing the proliferation of cancer cells and inducing cell apoptosis. This discovery has potential application value in the field of anti-cancer drug development.
Application in scientific research field
Molecular biology research: In molecular biology research, it is often used as a tool reagent to study biological processes such as protein synthesis, ribosome function, and gene expression regulation. By utilizing the inhibitory effect of Thiost, researchers can observe and analyze the functions and mechanisms of specific genes or proteins in cells. In addition, it can also be used to screen and identify genes or compounds related to ribosome function, providing powerful tools for a deeper understanding of ribosome structure and function.
Pharmacological research: In pharmacological research, it has been widely studied as a compound with anticancer activity. Researchers conducted in-depth studies on its effects on cancer cell proliferation, apoptosis, and tumor growth through in vitro and in vivo experiments. These studies not only reveal its anti-cancer mechanism, but also provide important basis for its application in the development of anti-cancer drugs. In addition, it can also serve as a model compound for drug screening, used to discover and develop novel drugs with similar anti-cancer activity.
What are the side effects of this compound?
Thiostrepton, as an antibiotic and protein synthesis inhibitor, has a wide range of applications in scientific research. However, like other drugs, it may also have some side effects during use:
1. Side effects
Discomfort in the digestive system
Some patients may experience digestive discomfort after receiving treatment with this compound. This mainly includes nausea, vomiting, diarrhea, etc. These symptoms are usually caused by the stimulating effect of drugs on the gastrointestinal mucosa. For patients experiencing digestive system discomfort, it is recommended to adjust the medication regimen, such as reducing the drug dosage or changing the administration time, to alleviate symptoms.
Allergic reactions
In rare cases, patients may develop allergic reactions to it. The symptoms of allergic reactions may include rash, itching, difficulty breathing, facial swelling, etc. Once an allergic reaction occurs, the medication should be stopped immediately and medical assistance sought. For patients with allergic constitution, an allergy test should be conducted before use to ensure safe use.
Symptoms of the nervous system
Its use may also cause some neurological symptoms, such as headaches, dizziness, etc. These symptoms may be related to the direct effects of medication on the nervous system. For patients with neurological symptoms, it is recommended to closely monitor changes in symptoms and adjust the dosing regimen or discontinue medication if necessary.
Impairment of liver and kidney function
Long term or excessive use may cause damage to liver and kidney function. Medications are metabolized and excreted in the liver and kidneys, and long-term or excessive use can increase the burden on the liver and kidneys, leading to abnormal liver and kidney function. Therefore, during use, liver and kidney function indicators such as transaminase and creatinine should be regularly monitored to promptly detect and treat liver and kidney function damage.
Abnormal blood system
Its use may also lead to abnormalities in the blood system, such as leukopenia, thrombocytopenia, etc. These symptoms may be related to the inhibitory effect of drugs on bone marrow hematopoietic function. For patients with hematological abnormalities, medication should be immediately discontinued and relevant tests should be performed to assess whether bone marrow hematopoietic function is impaired.
Other side effects
In addition to the common side effects mentioned above, the use of this substance may also cause some other side effects, such as fever, chills, fatigue, etc. These symptoms are usually mild, and as the medication time prolongs and the body gradually adapts, the symptoms will be relieved. However, for patients whose symptoms persist or worsen, timely medical attention and adjustment of treatment plans should be sought.
2.Preventive measures and treatment methods for side effects
preventive measure
- Strictly control the indications: Before using Thiostrepton, the patient's condition and physical condition should be carefully evaluated to ensure that the indications for drug use are clear.
- Standardized medication: strictly follow the dosage, usage, and course of treatment specified in the doctor's advice and instructions to avoid excessive use or abuse.
- Monitoring adverse reactions: During the use of medication, the patient's physical condition and adverse reactions should be closely monitored, and timely detection and treatment should be carried out.
- Special populations should use with caution: Pregnant women, breastfeeding women, children and other special populations should use with caution and under the guidance of a doctor.
processing method
- Discontinuation and observation: Once adverse reactions occur, the medication should be stopped immediately and symptoms should be closely monitored for changes. For patients with mild symptoms, they can self relieve after discontinuing the medication.
- Symptomatic treatment: For patients with severe symptoms, symptomatic treatment should be carried out according to the specific situation, such as using anti allergic drugs, hepatoprotective drugs, etc.
- Adjust treatment plan: For patients with serious adverse reactions, the treatment plan should be adjusted according to the doctor's advice, and other appropriate drugs or treatment methods should be selected.
3.Suggestions for safe use
To ensure the safe use of Thiostrepton, the following are some suggestions:
- Before use, carefully read the instructions and understand the indications, dosage, contraindications, and other information of the medication.
- Strictly follow the dosage, usage, and course of treatment specified in the doctor's advice and instructions to avoid overuse or misuse of the medication.
- During the use of medication, the patient's physical condition and adverse reactions should be closely monitored and reported to the doctor in a timely manner.
- For special populations such as pregnant women, breastfeeding women, children, etc., they should be used under the guidance of a doctor.
Scope of application and safety
Scope of Application: Diverse applications from laboratories to clinical Settings
Thiosrepton is a cyclic oligopeptide antibiotic derived from Streptomyces fargesii. Its unique chemical structure (including thiazole ring and polysulfide atom) endows it with multiple biological activities. Its application fields cover basic research, anti-tumor therapy and immune regulation:
Molecular biology tools
Recombinant screening marker: The methylase encoded by the Thiostrepton resistance gene (tsr) can specifically modify 23S rRNA, preventing drugs from binding to ribosomes, and thus serves as a screening marker for Streptomyces recombinant plasmids. This gene has been widely cloned into Streptomyces vector systems for genetic engineering operations.
Protein synthesis research: By inhibiting the binding of the 50S ribosome subunit to the elongation factor G (EF-G), and blocking the hydrolysis of GTP and the release of EF-G, Thiostrepton has become an important tool for studying the mechanism of bacterial protein synthesis.
Anti-tumor therapy
FOXM1 inhibitors: FOXM1 is a key transcription factor regulating the cell cycle and is overexpressed in various malignant tumors, such as colon cancer and breast cancer. Thiostrepton significantly inhibits tumor cell proliferation by down-regulating the expression of FOXM1.
In vitro experiments showed that it had a strong inhibitory effect on A2780 ovarian cancer cells (IC50=1.10 μM) and HEC-1A endometrial cancer cells (IC50=2.22 μM).
In animal models, intraperitoneal injection of 17 mg/kg could reduce the tumor volume of Ewing's sarcoma mice by approximately 72%, and no significant toxicity was observed.
Targeting advantage: Compared with traditional chemotherapy drugs, Thiostrepton has higher selectivity for rapidly proliferating tumor cells and fewer side effects.
Immune regulation
TLR7-9 inhibitors: Abnormal activation of Toll-like receptor 7-9 (TLR7-9) is closely related to autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus. Thiostrepton provides a new therapeutic strategy for immune disorder diseases by inhibiting the TLR7-9 signaling pathway and reducing the release of inflammatory factors.
Preclinical potential: In psoriasis-like inflammatory models, Thiostrepton significantly reduces skin inflammatory responses, and its targeting specificity is superior to that of the proteasome inhibitor bortezomib.
Exploration of New Applications
Scleroderma treatment: Recent studies have confirmed that Thiostrepton can improve the skin hardening symptoms of scleroderma by regulating fibrosis-related signaling pathways, providing an alternative for patients intolerant to immunosuppressants.
Antibacterial activity: As a Gram-positive bacteria inhibitor, Thiostrepton shows potential antibacterial effects against drug-resistant strains such as methicillin-resistant Staphylococcus aureus.
Safety Assessment: The Boundary between Research and Clinical Practice
Toxicity characteristics
Acute toxicity: Animal experiments have shown that intraperitoneal injection of 17 mg/kg does not cause severe organ damage, but high doses (such as 100 mg/kg) may cause mild hepatotoxicity.
Cytotoxicity: In vitro experiments have shown that the IC50 of Thiostrepton against normal cells (such as human fibroblasts) is significantly higher than that against tumor cells (>10 μM), suggesting a wider therapeutic window.
Long-term risk: Currently, there is no data on long-term human use, but no drug resistance or cumulative toxicity has been observed in animal models.
Operation and storage specifications
Personal protection: Gas masks, anti-static clothing and goggles must be worn to avoid inhalation of vapors or skin contact.
Solvent selection: It is recommended to use DMSO for dissolution (125 mg/mL), and avoid aqueous solutions (which are prone to precipitation).
Storage conditions: After aliquoting, store at -20℃ (for use within 1 month), or store at -80℃ for a long time (for 6 months). Avoid repeated freezing and thawing.
Clinical transformation challenges
Water solubility limitation: Thiostrepton is slightly soluble in water and its bioavailability needs to be improved through nanocarriers or chemical modifications (such as peG-ylation).
Administration route: Currently, intraperitoneal injection is mostly used in animal experiments. For clinical applications, oral or topical administration preparations need to be developed.
Regulatory status: As a research reagent, Thiostrepton is strictly prohibited from being used on the human body, and its clinical application must go through a strict drug approval process.
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