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4"-Isovalerylspiramycin I

(Synonyms: Isovalerylspiramycin I; Shengjimycin E)

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.

For research use only. We do not sell to patients.

CAS No.: 267662-22-6
Formula: C₄₈H₈₂N₂O₁₅
Molecular Weight:927.17

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (285 KB)

4"-Isovalerylspiramycin I Chemical Structure

CAS No.: 267662-22-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Top1

Chk1

All Topoisomerase Isoforms :

All DNA/RNA Synthesis Isoforms :

All Checkpoint Kinase (Chk) Isoforms :

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

143B and Saos-2
Concentration:

0-40 µM (143B, TOP1-overexpressing 143B); 0-50 µM (Saos-2, TOP1-overexpressing Saos-2)
Incubation Time:

24 h
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.

Cell Migration Assay^[1]

Cell Line:

143B and Saos-2
Concentration:

2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:

24 h
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.

Cell Invasion Assay^[1]

Cell Line:

143B and Saos-2
Concentration:

2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:

24 h (pre-treatment)
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.

Apoptosis Analysis^[1]

Cell Line:

143B and Saos-2
Concentration:

2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:

24 h
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).

Western Blot Analysis^[1]

Cell Line:

143B and Saos-2
Concentration:

2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:

24 h
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.

Cell Cycle Analysis^[1]

Cell Line:

143B and Saos-2
Concentration:

2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:

24 h
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.

In Vivo

4"-Isovalerylspiramycin I (Isovalerylspiramycin I) (60 mg/kg; i.p.; every 1 day; 30 days) significantly inhibits subcutaneous osteosarcoma tumor growth and lung metastasis in female M-NSG mice with good tolerability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

M-NSG mice (female, 4-6 weeks old, ~20 g) injected with 143B cells.^[1]
Dosage:

60 mg/kg
Administration:

i.p.; every 1 day; 30 days
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

CAS No. 267662-22-6
Molecular Weight 927.17
Formula C₄₈H₈₂N₂O₁₅
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
Synonyms

Isovalerylspiramycin I; Shengjimycin E
Structure Classification
- Others
Initial Source
- Microorganisms
S. spiramyceticus F21
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jinrong Liang, et al. Isovalerylspiramycin I inhibits proliferation, migration and invasion of osteosarcoma cells by targeting Topoisomerase 1 and suppressing the ataxia telangiectasia and Rad3-related/checkpoint kinase 1 pathway. Clin. Transl. Disc. 2023;3:e203.

[2]. Ma C, et al. Construction of 4"-isovalerylspiramycin-I-producing strain by in-frame partial deletion of 3-O-acyltransferase gene in Streptomyces spiramyceticus WSJ-1, the bitespiramycin producer. Curr Microbiol. 2011;62(1):16-20. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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4"-Isovalerylspiramycin I

All Topoisomerase Isoforms

All DNA/RNA Synthesis Isoforms

All Checkpoint Kinase (Chk) Isoforms