| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]
SKI-I targets human sphingosine kinase (SK), with an IC₅0 of 1.2 microM for ST-hSK. It also inhibits hERK2 with an IC₅0 of 11 microM. By inhibiting SK1 and SK2, SKI-I blocks the production of S1P, a bioactive lipid that promotes cell survival, proliferation, and inflammation. |
|---|---|
| ln Vitro |
SKI-I (Compound I; 5 μg/mL) 99% inhibits SK activity[1]. T24 cells are induced to undergo apoptosis by SKI-I (10 μM; 24 h)[1]
In vitro, SKI-I inhibits cell growth and induces apoptosis in cancer cell lines. It suppresses S1P production and promotes cell death. The compound also exhibits anti-inflammatory effects. SKI-I induces autophagy in treated cells, contributing to its antiproliferative effects. |
| ln Vivo |
In vivo, SKI-I has shown promising results in preclinical studies for cancer and inflammatory diseases. It is expected to suppress tumor growth through the inhibition of S1P-mediated survival signaling. Detailed in vivo efficacy data are limited and primarily derived from ongoing research studies.
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| Enzyme Assay |
Enzyme assays for SKI-I typically involve measuring sphingosine kinase activity using purified enzyme or cell lysates. The enzyme is incubated with sphingosine and ATP in the presence of varying concentrations of the inhibitor, and S1P production is quantified by mass spectrometry or radiometric methods.
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| Cell Assay |
Cell-based assays for SKI-I utilize various cancer cell lines to assess antiproliferative and pro-apoptotic effects. Cells are treated with the compound, and cell viability is measured using MTT or similar assays. Apoptosis is assessed by caspase activation or Annexin V staining. Autophagy markers such as LC3-II are also evaluated.
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| Animal Protocol |
In vivo studies with SKI-I are conducted in rodent models of cancer or inflammation. The compound is typically administered via intraperitoneal or oral administration. Tumor growth, inflammatory markers, and survival are monitored. S1P levels in tissues and plasma may also be measured.
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| ADME/Pharmacokinetics |
As a small molecule, SKI-I is expected to have reasonable pharmacokinetic properties. Standard pharmacokinetic studies would involve measuring plasma concentrations after administration and calculating parameters such as half-life, Cmax, and AUC. The compound should be stored under appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicity data for SKI-I are limited. Sphingosine kinase inhibitors may have effects on normal cellular functions due to the role of S1P in various physiological processes. Standard safety precautions for laboratory handling of research compounds should be followed.
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| References | |
| Additional Infomation |
SKI-I is a research-use compound and is not approved for therapeutic applications. It is a potent and selective inhibitor of human sphingosine kinase. The compound is used to study sphingolipid signaling, cancer biology, and inflammation. It is available from multiple research suppliers.
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| Molecular Formula |
C25H18N4O2
|
|---|---|
| Molecular Weight |
406.44
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| Exact Mass |
406.143
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| CAS # |
306301-68-8
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| PubChem CID |
135515522
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
5.243
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
655
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| Defined Atom Stereocenter Count |
0
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 100 mg/mL (246.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4604 mL | 12.3019 mL | 24.6039 mL | |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9208 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 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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