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| 5mg |
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| Targets |
Holomycin targets bacterial RNA polymerase, inhibiting DNA-dependent RNA synthesis. It also functions as a chelating agent. The compound's antibacterial activity is attributed to its inhibition of RNA polymerase, disrupting transcription and protein synthesis in susceptible organisms. It has antitumor activity and can act in vivo on RNA synthesis.
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| ln Vitro |
Holomycin demonstrates broad-spectrum antibacterial activity in vitro against Gram-positive and Gram-negative bacteria, fungi, and protozoa. It exhibits antitumor activity. The compound's mechanism involves inhibition of DNA-dependent RNA polymerase.
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| ln Vivo |
In vivo activity of holomycin includes antitumor activity, with the compound acting on RNA synthesis in vivo. Its broad-spectrum antibacterial activity suggests potential for treating bacterial infections in vivo, but further studies are needed to evaluate its pharmacokinetic properties and therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for holomycin involve measuring its inhibition of DNA-dependent RNA polymerase activity. The assay typically uses purified RNA polymerase and measures the incorporation of radiolabeled nucleotides into RNA in the presence of the compound. Inhibition of RNA synthesis is quantified, and IC50 values are determined.
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| Cell Assay |
In vitro cellular assays for holomycin involve culturing bacterial or fungal cells in the presence of varying concentrations of the compound. Antimicrobial activity is assessed by measuring inhibition of growth using optical density measurements or colony counting. Antitumor activity can be assessed using cancer cell lines.
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| Animal Protocol |
In vivo animal experiments for holomycin would typically involve administering the compound to animal models of bacterial infection or cancer. Efficacy is evaluated by measuring bacterial load in tissues, tumor growth inhibition, or survival rates. The compound's antitumor activity has been demonstrated in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for holomycin are limited. As a small heterocyclic antibiotic, its absorption, distribution, metabolism, and excretion properties would influence its bioavailability. Further pharmacokinetic studies are needed to determine its systemic exposure and elimination pathways.
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| Toxicity/Toxicokinetics |
Toxicological data for holomycin are limited. As a broad-spectrum antibiotic, it may have potential for toxicity at higher concentrations. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only.
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| References | |
| Additional Infomation |
Holomycin is a dithiopyrrolidone antibiotic with the chemical name 4,5-dihydro[1,2]dithio[4,3-b]pyrrole, in which the hydrogen atoms at positions 5 and 6 are replaced by oxo groups and acetamide groups, respectively. It is a DNA-dependent RNA polymerase inhibitor with antibacterial and antitumor activities. It functions as a chelating agent, antitumor drug, EC 2.7.7.6 (RNA polymerase) inhibitor, antibacterial agent, marine metabolite, and bacterial metabolite. It is a dithiopyrrolidone antibiotic belonging to the acetamide class of compounds. Holomycin has been reported in Streptomyces, Yersinia rumeni, and other organisms with relevant data.
Holomycin (CAS#: 488-04-0) has the molecular formula C7H6N2O2S2 and a molecular weight of 214.26 g/mol. Its IUPAC name is N-(5-oxo-4H-dithiolo[4,3-b]pyrrol-6-yl)acetamide. The compound is a DNA-dependent RNA polymerase inhibitor with antibacterial and antitumor activities. |
| Molecular Formula |
C7H6N2O2S2
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|---|---|
| Molecular Weight |
214.26
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| Exact Mass |
213.987
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| Elemental Analysis |
C, 39.24; H, 2.82; N, 13.07; O, 14.93; S, 29.93
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| CAS # |
488-04-0
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| PubChem CID |
10262683
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| Appearance |
Solid powder
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| Density |
1.632g/cm3
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| Boiling Point |
532.147ºC at 760 mmHg
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| Flash Point |
275.633ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.742
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| LogP |
2.622
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
360
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)NC1=C2C(=CSS2)NC1=O
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| InChi Key |
HBUNPJGMNVQSBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H6N2O2S2/c1-3(10)8-5-6-4(2-12-13-6)9-7(5)11/h2H,1H3,(H,8,10)(H,9,11)
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| Chemical Name |
N-(5-oxo-4H-dithiolo[4,3-b]pyrrol-6-yl)acetamide
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| Synonyms |
Holomycin
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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: Please store this product in a sealed and protected environment, 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.6672 mL | 23.3361 mL | 46.6723 mL | |
| 5 mM | 0.9334 mL | 4.6672 mL | 9.3345 mL | |
| 10 mM | 0.4667 mL | 2.3336 mL | 4.6672 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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