4"-Isovalerylspiramycin I
4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection.
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- CAS No.: 267662-22-6
- Formule: C48H82N2O15
- Masse moléculaire:927.17
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Stockage:
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4"-Isovalerylspiramycin I (0-50 µM; 24 h) dose-dependently inhibits the proliferation of 143B and Saos-2 human osteosarcoma cells after 24 h incubation, with IC50 values of 8.7 µM and 17.8 µM respectively; this effect is reversed by TOP1 overexpression[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h) dose-dependently inhibits the migration of 143B and Saos-2 human osteosarcoma cells after 24 h incubation; this effect is reversed by TOP1 overexpression[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h pre-treatment) dose-dependently inhibits the invasion of 143B and Saos-2 human osteosarcoma cells after 24 h pre-treatment; this effect is reversed by TOP1 overexpression[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h) dose-dependently inhibits DNA replication in 143B and Saos-2 human osteosarcoma cells after 24 h incubation, as measured by reduced EdU incorporation[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h) dose-dependently induces apoptosis in 143B and Saos-2 human osteosarcoma cells after 24 h incubation[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h) dose-dependently alters the expression of pro- and anti-apoptotic proteins in 143B and Saos-2 human osteosarcoma cells after 24 h incubation[1].
4"-Isovalerylspiramycin I (2.5-20 µM; 24 h) dose-dependently reduces the expression of G0/G1 cell cycle regulatory proteins in 143B and Saos-2 human osteosarcoma cells after 24 h incubation[1].
4"-Isovalerylspiramycin I (10-20 µM; 18 h) directly binds to intracellular TOP1 in 143B and Saos-2 human osteosarcoma cells, increasing TOP1 thermal stability after 18 h incubation[1].
4"-Isovalerylspiramycin I (0.125 μg/mL) inhibits methicillin-resistant Staphylococcus aureus CMCC 5342 with an MIC of 0.125 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:143B and Saos-2
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Concentration:0-40 µM (143B, TOP1-overexpressing 143B); 0-50 µM (Saos-2, TOP1-overexpressing Saos-2)
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Incubation Time:24 h
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Result:Inhibited 143B and Saos-2 cell proliferation in a dose- and time-dependent manner, with IC50 values of 8.7 µM (143B) and 17.8 µM (Saos-2) after 24 h.
Increased IC50 values to 19.2 µM (TOP1-overexpressing 143B) and 30.6 µM (TOP1-overexpressing Saos-2) after 24 h, reversing the antiproliferative effect.
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Cell Line:143B and Saos-2
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Concentration:2.5-10 µM (143B); 5-20 µM (Saos-2)
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Incubation Time:24 h
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Result:Reduced wound closure in both 143B and Saos-2 cells in a dose-dependent manner, inhibiting cell migration.
Reversed this inhibitory effect on migration when TOP1 was overexpressed.
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Cell Line:143B and Saos-2
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Concentration:2.5-10 µM (143B); 5-20 µM (Saos-2)
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Incubation Time:24 h (pre-treatment)
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Result:Reduced the number of invading 143B and Saos-2 cells in a dose-dependent manner.
Reversed this inhibitory effect on invasion when TOP1 was overexpressed.
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Cell Line:143B and Saos-2
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Concentration:2.5-10 µM (143B); 5-20 µM (Saos-2)
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis in both 143B and Saos-2 cells, with apoptosis rates reaching ~30% (143B at 10 µM) and ~30% (Saos-2 at 20 µM).
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Cell Line:143B and Saos-2
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Concentration:2.5-10 µM (143B); 5-20 µM (Saos-2)
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Incubation Time:24 h
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Result:Downregulated BCL-2 protein expression and upregulated cleaved caspase-3 and BAX protein expression in both 143B and Saos-2 cells in a dose-dependent manner.
Reduced protein expression of CDK4 and Cyclin D1 in both 143B and Saos-2 cells in a dose-dependent manner.
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Cell Line:143B and Saos-2
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Concentration:2.5-10 µM (143B); 5-20 µM (Saos-2)
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in the percentage of cells in the G0/G1 phase, with a corresponding decrease in the S-phase population in both 143B and Saos-2 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:M-NSG mice (female, 4-6 weeks old, ~20 g) injected with 143B cells.[1]
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Dosage:60 mg/kg
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Administration:i.p.; every 1 day; 30 days
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Result:Significantly inhibited increases in tumor volume in 143B xenografts.
Showed no significant difference in mouse body weight compared to controls, indicating good tolerability.
Reduced TOP1 expression in tumor tissues via immunohistochemical staining.
Significantly inhibited osteosarcoma lung metastasis via lung H&E staining.
Chemical Information
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CAS No. 267662-22-6
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Masse moléculaire 927.17
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Formule C48H82N2O15
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SMILES
O=CC[C@@H](C[C@H]([C@H](/C=C/C=C/C[C@H](OC(C[C@H]([C@@H]1OC)O)=O)C)O[C@@H]2O[C@@H]([C@H](CC2)N(C)C)C)C)[C@@H]1O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)C)O[C@H]4C[C@@](O)([C@H]([C@@H](O4)C)OC(CC(C)C)=O)C)N(C)C)O
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Synonyms
Isovalerylspiramycin I; Shengjimycin E
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Structure Classification
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Initial Source
S. spiramyceticus F21
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
4"-Isovalerylspiramycin I Related Classifications
HY-N15249 Related Classifications
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- 4"-Isovalerylspiramycin I
- 267662-22-6
- Isovalerylspiramycin I
- Shengjimycin E
- Topoisomerase
- DNA/RNA Synthesis
- Checkpoint Kinase (Chk)
- Apoptosis
- Bacterial
- TOP1
- osteosarcoma cells
- CHEK1
- methicillin-resistant Staphylococcus aureus
- apoptosis
- ATR/CHEK1 pathway
- DNA replication
- tumour xenograft mouse model
- DNA damage
- cell cycle arrest
- Inhibitor
- inhibitor
- inhibit