2. Cell Cycle/DNA Damage Apoptosis Anti-infection
  3. Topoisomerase DNA/RNA Synthesis Checkpoint Kinase (Chk) Apoptosis Bacterial
  4. 4"-Isovalerylspiramycin I

4"-Isovalerylspiramycin I  (Synonyms: Isovalerylspiramycin I; Shengjimycin E)

Cat. No.: HY-N15249
Handling Instructions Technical Support

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.

4

4"-Isovalerylspiramycin I Chemical Structure

CAS No. : 267662-22-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

4"-Isovalerylspiramycin I Related Antibodies

Top Publications Citing Use of Products

View All Topoisomerase Isoform Specific Products:

View All Isoforms
Topoisomerase Topo I Topo II DNA gyrase

View All DNA/RNA Synthesis Isoform Specific Products:

View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

View All Checkpoint Kinase (Chk) Isoform Specific Products:

View All Isoforms
Chk1 Chk2 BUBR1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

Top1

 

Chk1

 

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.

4"-Isovalerylspiramycin I Related Antibodies

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.
Molecular Weight

927.17

Formula

C48H82N2O15
CAS No.
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
Structure Classification
Initial Source

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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

4"-Isovalerylspiramycin I Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

4"-Isovalerylspiramycin I267662-22-6Isovalerylspiramycin I Shengjimycin ETopoisomeraseDNA/RNA SynthesisCheckpoint Kinase (Chk)ApoptosisBacterialTOP1osteosarcoma cellsCHEK1methicillin-resistant Staphylococcus aureusapoptosisATR/CHEK1 pathwayDNA replicationtumour xenograft mouse modelDNA damagecell cycle arrestInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
4"-Isovalerylspiramycin I
Cat. No.:
HY-N15249
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.