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Thiostrepton

Name: Thiostrepton
Brand: Selleck Chemicals
SKU: S4354
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S4354

Thiostrepton (Alaninamide, Bryamycin, Thiactin) is a natural cyclic oligopeptide antibiotic, derived from several strains of strepromycetes.

Chemical Structure

Molecular Weight: 1664.89

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	PROTAC Dyes Antineoplastic and Immunosuppressive Antibiotics ADC Cytotoxin Selection Antibiotics for Transfected Cell Antibiotics for Mammalian Cell Culture ADC Linker Molecular Glues Antibiotics for Plant Cell Culture PROTAC Linker
Other Others Inhibitors	BAY 2927088（Sevabertinib） Guanidinoacetic acid BAPTA-AM Blebbistatin Methyl-β-cyclodextrin (MβCD) Carbazochrome sodium sulfonate (AC-17) Ursolic Acid Osthole 4-Methylumbelliferone (4-MU) Dioscin

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (0.75mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (3.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (0.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	1664.89	Formula	C₇₂H₈₅N₁₉O₁₈S₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1393-48-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Alaninamide, Bryamycin, Thiactin			Smiles	CCC(C)C1C(=O)NC(C(=O)NC(=C)C(=O)NC(C(=O)NC23CCC(=NC2C4=CSC(=N4)C(C(OC(=O)C5=NC6=C(C=CC(C6O)N1)C(=C5)C(C)O)C)NC(=O)C7=CSC(=N7)C(NC(=O)C8CSC(=N8)C(=CC)NC(=O)C(NC(=O)C9=CSC3=N9)C(C)O)C(C)(C(C)O)O)C1=NC(=CS1)C(=O)NC(=C)C(=O)NC(=C)C(=O)N)C)C

Mechanism of Action

In vitro

Thiostrepton inhibits growth of the parasite in the micromolar range which is 10-fold below concentrations with observable effects on total protein synthesis. This compound results in disappearance of organellar-encoded RNA transcripts within 6 hours of treatment while transcripts of a nuclear-encoded mRNA remain constant for at least 8 hous of treatment. It directly interacts with two nucleotides in the GTPase domain of Escherichia coli. This chemical directly interacts the region around position 1067 in domain II of 23S rRNA inhibits GTP hydrolysis by elongation factor G (EF-G) on the ribosome at the conditions of multiple turnover. It interferes with EF-G footprints in the alpha-sarcin stem loop (A2660, A2662) located in domain VI of 23S rRNA. The compound interacts with a 58-nucleotide domain of large subunit ribosomal RNA, and binds to the ribosome cooperatively with Ribosomal protein L11. Its and RNA recognition cooperativity can be attributed to N- and C-terminal domains of L11, respectively. It binds primarily to 23 S rRNA, thus probably inhibits peptide elongation by impeding a conformational change within protein L11 that is important for the function of the ribosomal GTPase centre. Treatment with this compound (10 μM) reduces FOXM1 expression in a time- and dose-dependent manner, independent of de novo protein synthesis and predominantly at transcriptional and gene promoter levels. It (10 μM) induces cell cycle arrest at G(1) and S phases and cell death, concomitant with FOXM1 repression in breast cancer cells. This agent (10 μM) also shows efficacy in repressing breast cancer cell migration, metastasis, and transformation, which are all downstream functional attributes of FOXM1.

References

[1] https://pubmed.ncbi.nlm.nih.gov/8999899/
[2] https://pubmed.ncbi.nlm.nih.gov/10449736/
[3] https://pubmed.ncbi.nlm.nih.gov/8634289/

[4] https://pubmed.ncbi.nlm.nih.gov/9512711/
[5] https://pubmed.ncbi.nlm.nih.gov/18645012/

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