| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The primary target of Sparsomycin is the peptidyl transferase center (PTC) of the 50S ribosomal subunit. It binds to the PTC and inhibits peptide bond formation, blocking protein synthesis. Sparsomycin also inhibits the binding of aminoacyl-tRNA to the ribosomal A-site. The compound has a unique binding site that overlaps with but is distinct from those of other PTC inhibitors. Its broad-spectrum activity against both prokaryotic and eukaryotic ribosomes makes it a valuable research tool.
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|---|---|
| ln Vitro |
In vitro, Sparsomycin inhibits protein synthesis in both prokaryotic and eukaryotic cell-free systems with IC50 values in the low micromolar range. It inhibits the growth of various bacterial strains and cancer cell lines. The compound is used as a research tool for studying ribosome structure and function, particularly the peptidyl transferase center. It is typically tested at concentrations ranging from 0.1 to 100 μM.
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| ln Vivo |
In vivo, Sparsomycin has been evaluated in preclinical animal models for antitumor and antibacterial activity. Its clinical development was limited by toxicity, including bone marrow suppression and gastrointestinal toxicity. Specific published in vivo efficacy data are limited. Sparsomycin is primarily used as a research tool for studying translation and as a reference compound for ribosome-targeting antibiotics.
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| Enzyme Assay |
The protein synthesis inhibition assay uses cell-free translation systems (e.g., E. coli or rabbit reticulocyte lysates) programmed with mRNA. Sparsomycin is added at serial dilutions. Protein synthesis is measured by incorporation of radiolabeled amino acids (e.g., [³⁵S]methionine) into trichloroacetic acid-precipitable material. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, bacterial cultures or cancer cell lines are treated with serial dilutions of Sparsomycin. Bacterial growth inhibition is measured by optical density or colony-forming units. Cancer cell viability is assessed using MTT or CellTiter-Glo reagent. Protein synthesis in cells is measured by [³⁵S]methionine incorporation. Ribosome binding is assessed by sucrose gradient centrifugation.
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| Animal Protocol |
In vivo studies with Sparsomycin would employ mouse models of infection or cancer. The compound is dissolved in saline or appropriate vehicle and administered intraperitoneally or intravenously. Doses are selected based on toxicity studies. Key readouts include tumor growth inhibition, bacterial burden in tissues, and survival. Due to toxicity, in vivo studies are limited and primarily used for mechanistic investigations.
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| References | |
| Additional Infomation |
Reports have indicated the discovery of sclerotinib in Streptomyces sparserum, a species of Streptomyces, and relevant data are available. Streptomyces sparserum produces an antitumor antibiotic. It inhibits protein synthesis in the 70S and 80S ribosomal systems.
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| Molecular Formula |
C13H19N3O5S2
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|---|---|
| Molecular Weight |
361.431
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| Exact Mass |
361.077
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| CAS # |
1404-64-4
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| PubChem CID |
9543443
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| Appearance |
White to off-white solid powder
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| Density |
1.466g/cm3
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| Index of Refraction |
1.656
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| LogP |
0.187
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
574
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CSCS(C[C@@H](NC(/C=C/C1=C(C)NC(=O)NC1=O)=O)CO)=O
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| InChi Key |
XKLZIVIOZDNKEQ-CLQLPEFOSA-N
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| InChi Code |
InChI=1S/C13H19N3O5S2/c1-8-10(12(19)16-13(20)14-8)3-4-11(18)15-9(5-17)6-23(21)7-22-2/h3-4,9,17H,5-7H2,1-2H3,(H,15,18)(H2,14,16,19,20)/b4-3+/t9-,23+/m0/s1
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| Chemical Name |
(E)-N-[(2S)-1-hydroxy-3-[(R)-methylsulfanylmethylsulfinyl]propan-2-yl]-3-(6-methyl-2,4-dioxo-1H-pyrimidin-5-yl)prop-2-enamide
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| Synonyms |
U-19183; U 19183; Sparsomycin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~1 mg/mL (~2.8 mM; with ultrasonication and warming)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7668 mL | 13.8339 mL | 27.6679 mL | |
| 5 mM | 0.5534 mL | 2.7668 mL | 5.5336 mL | |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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