| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
SKI V does not inhibit PKC-α and has weak activity against ERK2 (IC50 for hERK2 is 80 μM)[1]. SKI V (10 μM; for 24 hours) causes apoptosis and suppresses the growth of cancer cells [1]. SKI V decreased the levels of phospho-Akt and phospho-MEK (0.2, 1, 5 μM; 1 hour pretreatment). After 16 hours of serum starvation, near-confluent JC cell cultures received a 1-hour SKI V pretreatment [2]. SKI V suppresses the growth of tumor cells and sphingosine kinase (SK) at an IC50 of approximately 2 μM [1]. In MDA-MB-231 cells, SKI V (20 μg/ml) suppresses both endogenous and purified SK [1]. In JC cells, SKI V (0.2, 1, 5 μM) suppresses the production of intracellular S1P in a dose-dependent manner [2].
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|---|---|
| ln Vivo |
In comparison with control rats, SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly slowed tumor growth (reduction of >50% on day 18) [1].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: T24 tumor cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cancer cell proliferation. Apoptosis analysis[1] Cell Types: T24 tumor cells Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis. Western Blot Analysis[2] Cell Types: JC Cell Tested Concentrations: 0.2, 1, 5 μM Incubation Duration: 1 hour pretreatment Experimental Results: diminished levels of phospho-Akt and phospho-MEK. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old BALB/c female mice, JC breast cancer cells [1]
Doses: 75 mg/kg Route of Administration: IP; results on days 1, 5, 9, and 15: compared with control animals Tumor growth was Dramatically diminished (>50% reduction on day 18) compared with tumor growth. |
| References | |
| Additional Infomation |
3',4'-dihydroxyaurone is a hydroxyaurone that is aurone which is substituted by hydroxy groups at the 3' and 4' positions; major species at pH 7.3. It shows inhibitory activity against several isoforms of the histone deacetylase complex (HDAC). It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a hydroxyaurone and a member of catechols. It is functionally related to a 2',3,4-trihydroxy-trans-chalcone.
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| Molecular Formula |
C15H10O4
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|---|---|
| Molecular Weight |
254.2375
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| Exact Mass |
254.057
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| CAS # |
24418-86-8
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| PubChem CID |
5793932
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.9
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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 |
19
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(=C([H])C2C([H])=C([H])C(=C(C=2[H])O[H])O[H])C(C2=C([H])C([H])=C([H])C([H])=C12)=O
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| InChi Key |
HCBULGQMULJTCM-ZSOIEALJSA-N
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| InChi Code |
InChI=1S/C15H10O4/c16-11-6-5-9(7-12(11)17)8-14-15(18)10-3-1-2-4-13(10)19-14/h1-8,16-17H/b14-8-
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| Chemical Name |
(2Z)-2-[(3,4-dihydroxyphenyl)methylidene]-1-benzofuran-3-one
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| Synonyms |
SKI V; SKI-V
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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 : ~50 mg/mL (~196.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL | |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL | |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 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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