| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 250mg |
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Purity: ≥98%
Bikinin (also known as Abrasin), a pyridinylamido compound, is a novel, potent, non-steroidal and ATP-competitive inhibitor of Arabidopsis GSK-3 (Glycogen synthase kinase 3). Additionally, it stimulates brassinosteroid (BR) signaling. Glycogen synthase kinase 3 (GSK3) is a crucial signaling pathway regulator in both plants and animals. It has been demonstrated that three Arabidopsis thaliana GSK3s are involved in brassinosteroid (BR) signaling.
| Targets |
GSK-3
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|---|---|
| ln Vitro |
Bikinin activates brassinosteroid-dependent gene expression by directly targeting BIN2 of Arabidopsis GSK-3s. [1] A 150 mM NaCl induction of GUS activity in the RD26pro:GUS line is also inhibited by bikinin, along with the expression of RD26. [3]
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| ln Vivo |
In vivo, bikinin inhibits T180 phosphorylation of SnRK2.3 and its kinase activity as well as the outputs of the abscisic acid signaling pathway. [2]
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| Enzyme Assay |
In Escherichia coli BL21, ASKs are expressed as GST-fusion proteins. In vitro kinase assays are carried out by incubating 50 ng of GST-fusion protein, 10 μg of myelin basic protein (MBP), and 0.15 MBq of γ-[32P]-ATP for 30 min at 25 °C. The reaction buffer is composed of 1 mM dithiothreitol, 20 mM HEPES/KOH pH 7.4, 15 mM MgCl2, 5 mM EGTA, and 1 μM cold ATP. Using an Amersham storage phosphor imager screen and a Biorad Molecular Imager FX, the reaction products are separated by SDS-PAGE, and the radioactivity incorporated into MBP is quantified.
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| Cell Assay |
To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number was determined every 24 h. Cells were exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h.
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| Animal Protocol |
NA;
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| References |
| Molecular Formula |
C9H9BRN2O3
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|---|---|
| Molecular Weight |
273.0834
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| Exact Mass |
271.97965
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| Elemental Analysis |
C, 39.58; H, 3.32; Br, 29.26; N, 10.26; O, 17.58
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| CAS # |
188011-69-0
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| Related CAS # |
188011-69-0
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| Appearance |
Solid powder
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| SMILES |
BrC1=CN=C(NC(CCC(O)=O)=O)C=C1
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| InChi Key |
XFYYQDHEDOXWGA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H9BrN2O3/c10-6-1-2-7(11-5-6)12-8(13)3-4-9(14)15/h1-2,5H,3-4H2,(H,14,15)(H,11,12,13)
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| Chemical Name |
4-((5-bromopyridin-2-yl)amino)-4-oxobutanoic acid; Abrasin;
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| Synonyms |
Bikinin
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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: ~54 mg/mL (~197.7 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 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 (9.15 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 | 3.6619 mL | 18.3097 mL | 36.6193 mL | |
| 5 mM | 0.7324 mL | 3.6619 mL | 7.3239 mL | |
| 10 mM | 0.3662 mL | 1.8310 mL | 3.6619 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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