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| Targets |
SPK-601 targets phosphatidylcholine-specific phospholipase C (PC-PLC), an enzyme that hydrolyzes phosphatidylcholine to generate second messengers involved in cell signaling. By inhibiting PC-PLC, SPK-601 disrupts lipid signaling pathways that are essential for cell growth and proliferation, as well as viral replication.
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| ln Vitro |
Inhibiting HPV-31-specific RNA expression and DNA replication, SPK-601 (72 hours; HPV-31 cells) shows a dose-dependent inhibitory effect on cell growth (IC50 of 16 μg/mL) [2].
SPK-601 is a potent PC-PLC inhibitor and antimicrobial agent. It shows a dose-dependent inhibitory effect on cell growth in HPV-31 cells with an IC50 of 16 μg/mL at 72 hours. SPK-601 also inhibits HPV-31 specific RNA expression and DNA replication. |
| ln Vivo |
Specific in vivo efficacy data for SPK-601 are not extensively detailed in standard reference sources. As a PC-PLC inhibitor with antimicrobial and antiviral activity, it would be expected to show efficacy in animal models of viral infections or cancer. Studies in HPV-related disease models would be required to fully characterize its in vivo effects.
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| Enzyme Assay |
SPK-601's inhibition of PC-PLC can be assessed using in vitro enzyme activity assays. Recombinant or purified PC-PLC enzyme is incubated with its substrate (phosphatidylcholine) in the presence of varying concentrations of SPK-601. The production of diacylglycerol or phosphocholine is measured using a suitable detection method (e.g., ELISA, radiometric, or fluorescence assay) to determine the IC50.
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| Cell Assay |
Cell viability assay [2]
Cell Types: 9E human papillomavirus (HPV)-31-infected cervical epithelial cells Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: Dose-dependent inhibition of cell growth. The cellular activity of SPK-601 is evaluated in HPV-31 cells or other cell lines. Cells are treated with increasing concentrations of SPK-601 for 72 hours, and cell viability is assessed using MTT or CellTiter-Glo assays. HPV-31 specific RNA expression is measured by RT-PCR, and DNA replication is assessed by quantifying viral DNA. |
| Animal Protocol |
SPK-601 would be administered via intraperitoneal or oral routes in animal models of HPV-related diseases or infections. Viral load, tumor growth, and immune responses would be assessed to evaluate efficacy. Specific in vivo animal experimental protocols are not extensively detailed in standard reference sources.
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| ADME/Pharmacokinetics |
SPK-601 potassium has a molecular formula of C11H15KOS2 and a molecular weight of 266.46 g/mol. Its chemical name is potassium O-[(3aR,4R,5S,7R,7aR)-octahydro-1H-4,7-methanoinden-5-yl] carbonodithioate. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of SPK-601 is not extensively documented. As a PC-PLC inhibitor, potential adverse effects may include disruption of lipid signaling in various tissues. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
SPK-601 potassium (CAS# 1096687-52-3) is also known as LMV-601. It is a cell-permeable inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC) and a useful antimicrobial agent. SPK-601 shows dose-dependent inhibition of cell growth and HPV-31 replication.
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| Molecular Formula |
C11H15KOS2
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|---|---|
| Molecular Weight |
266.4583
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| Exact Mass |
266.02
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| CAS # |
1096687-52-3
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| PubChem CID |
46909535
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.659
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
271
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1C[C@H]2[C@@H](C1)[C@H]3C[C@@H]2C[C@@H]3OC(=S)[S-].[K+]
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| InChi Key |
IGULCCCBGBDZKQ-UATZLORTSA-M
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| InChi Code |
InChI=1S/C11H16OS2.K/c13-11(14)12-10-5-6-4-9(10)8-3-1-2-7(6)8;/h6-10H,1-5H2,(H,13,14);/q;+1/p-1/t6-,7-,8-,9-,10+;/m1./s1
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| Chemical Name |
potassium;[(1R,2R,6R,7R,8S)-8-tricyclo[5.2.1.02,6]decanyl]oxymethanedithioate
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| Synonyms |
LM-601 SPK601 LMV601 SPK 601 LMV-601
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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 |
| 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) |
DMSO : ≥ 1 mg/mL (~3.75 mM)
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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 | 3.7529 mL | 18.7645 mL | 37.5291 mL | |
| 5 mM | 0.7506 mL | 3.7529 mL | 7.5058 mL | |
| 10 mM | 0.3753 mL | 1.8765 mL | 3.7529 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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