| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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2-D08, a synthetic flavone, is a cell permeable inhibitor of protein sumoylation that has a unique mechanism of action. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. Protein sumoylation is a dynamic posttranslational modification involved in diverse biological processes during cellular homeostasis and development. Sumoylation has been shown to play a critical role in cancer. 2-D08 showed anti-aggregatory and neuroprotective effect and may be used for the treatment of related diseases.
| Targets |
Axl(IC50= 0.49 nM)
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| ln Vitro |
2-D08, a synthetic flavone, is a cell permeable inhibitor of protein sumoylation that has a unique mechanism of action. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. Protein sumoylation is a dynamic posttranslational modification involved in diverse biological processes during cellular homeostasis and development. Sumoylation has been shown to play a critical role in cancer. 2-D08 showed anti-aggregatory and neuroprotective effect and may be used for the treatment of related diseases.
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| ln Vivo |
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| Enzyme Assay |
2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. IC50 values of the Axl kinase inhibitor (2D08) are determined using kinase-mediated phosphorylation of poly-GAT by AlphaScreen luminescence detection technology. The inhibitor is tested at eight points of dilution in duplicate.
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| Cell Assay |
Human lung multi-potent cells at passage 5 are plated at a density of 250 000 cells per well in six-well plates with growth medium. After 24 h, multi-potent cells are incubated with DMEM+0.5% BSA+penicillin/streptomycin containing 0.1% DMSO (vehicle) or 2D08 (0.1, 1, 10 μM) for 3 h in a humidified 5% CO2 incubator at 37℃. These cells are trypsinized and seeded at 20 000 cells per well in three replicates on 12-well cell culture transwell inserts with 8 μm pore size with DMEM+0.5% BSA+penicillin/streptomycin. Lower transwell chambers contained DMEM+10% FBS+penicillin/streptomycin are used to allow cells to migrate. 0.1% DMSO or 2D08 is added to corresponding upper and lower transwell chambers. After 16 h, non-migrated cells are removed by cotton swabs. Migrated cells are fixed with 4% PFA, permeabilized with methanol and stained with crystal violet. The field-images per transwell are taken by an inverted light microscope.
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| Animal Protocol |
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| References |
| Molecular Formula |
C15H10O5
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| Molecular Weight |
270.24
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| Exact Mass |
270.052
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| Elemental Analysis |
C, 66.67; H, 3.73; O, 29.60
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| CAS # |
144707-18-6
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| Related CAS # |
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| PubChem CID |
22507438
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
517.9±50.0 °C at 760 mmHg
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| Flash Point |
201.7±23.6 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
2.77
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2C(C=C(C3=C(O)C(O)=C(O)C=C3)OC=2C=C1)=O
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| InChi Key |
JJAXTFSPCLZPIW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O5/c16-10-6-5-9(14(18)15(10)19)13-7-11(17)8-3-1-2-4-12(8)20-13/h1-7,16,18-19H
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| Chemical Name |
2-(2,3,4-trihydroxyphenyl)-4H-1-benzopyran-4-one
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| Synonyms |
2-D08; 2D08; 2 D08.
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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. |
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| 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 : 54~150 mg/mL ( 199.82~555.06 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.25 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 (9.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | |
| 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | |
| 10 mM | 0.3700 mL | 1.8502 mL | 3.7004 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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