Thiostrepton

製品コードS4354 バッチS435403

印刷

化学情報

Synonyms

Alaninamide, Bryamycin, Thiactin

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₇₂H₈₅N₁₉O₁₈S₅

分子量

1664.89

CAS No.

1393-48-2

Solubility (25°C)*

体外

DMSO

50 mg/mL (30.03 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

1.25mg/ml

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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Thiostrepton (Alaninamide, Bryamycin, Thiactin) is a natural cyclic oligopeptide antibiotic, derived from several strains of strepromycetes.
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. Thiostrepton 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. Thiostrepton directly interacts with two nucleotides in the GTPase domain of Escherichia coli. ^[1] Thiostrepton 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. Thiostrepton interferes with EF-G footprints in the alpha-sarcin stem loop (A2660, A2662) located in domain VI of 23S rRNA. ^[2] Thiostrepton interacts with a 58-nucleotide domain of large subunit ribosomal RNA, and binds to the ribosome cooperatively with Ribosomal protein L11. Thiostrepton and RNA recognition cooperativity can be attributed to N- and C-terminal domains of L11, respectively. ^[3] Thiostrepton 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. ^[4] Thiostrepton (10 μM) treatment reduces FOXM1 expression in a time- and dose-dependent manner, independent of de novo protein synthesis and predominantly at transcriptional and gene promoter levels. Thiostrepton (10 μM) induces cell cycle arrest at G(1) and S phases and cell death, concomitant with FOXM1 repression in breast cancer cells. Thiostrepton (10 μM) also shows efficacy in repressing breast cancer cell migration, metastasis, and transformation, which are all downstream functional attributes of FOXM1. ^[5]

製品説明

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

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. Thiostrepton 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. Thiostrepton directly interacts with two nucleotides in the GTPase domain of Escherichia coli. ^[1] Thiostrepton 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. Thiostrepton interferes with EF-G footprints in the alpha-sarcin stem loop (A2660, A2662) located in domain VI of 23S rRNA. ^[2] Thiostrepton interacts with a 58-nucleotide domain of large subunit ribosomal RNA, and binds to the ribosome cooperatively with Ribosomal protein L11. Thiostrepton and RNA recognition cooperativity can be attributed to N- and C-terminal domains of L11, respectively. ^[3] Thiostrepton 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. ^[4] Thiostrepton (10 μM) treatment reduces FOXM1 expression in a time- and dose-dependent manner, independent of de novo protein synthesis and predominantly at transcriptional and gene promoter levels. Thiostrepton (10 μM) induces cell cycle arrest at G(1) and S phases and cell death, concomitant with FOXM1 repression in breast cancer cells. Thiostrepton (10 μM) also shows efficacy in repressing breast cancer cell migration, metastasis, and transformation, which are all downstream functional attributes of FOXM1. ^[5]

プロトコル(参考用のみ)

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Selective BD2 Inhibitor Exerts Anti-Fibrotic Effects via BRD4/FoxM1/Plk1 Axis in Orbital Fibroblasts From Patients With Thyroid Eye Disease [ Invest Ophthalmol Vis Sci, 2023, 64(7):9]	PubMed: 37272763
Targetable vulnerability of deregulated FOXM1/PLK1 signaling axis in diffuse large B cell lymphoma [ Am J Cancer Res, 2022, 12(10:4666-4679)]	PubMed: 36381323
Thiostrepton reactivates latent HIV-1 through p-TEFb and NF-κB pathway mediated by heat shock response. [ Antimicrob Agents Chemother, 2020, 10.1128/AAC.02328-19]	PubMed: 32094131

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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