product name Bikinin
Description: Bikinin is a potent Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling. Bikinin directly binds the GSK3 BIN2 and acts as an ATP competitor. Bikinin inhibits the activity of six other Arabidopsis GSK3s. Glycogen synthase kinase 3 (GSK3) is a key regulator in signaling pathways in both animals and plants. Plant GSK-3/Shaggy-like kinases are key players in brassinosteroid (BR) signalling which impact on plant development and participate in response to wounding, pathogens and salt stress.
References: Mol Cells. 2014 Nov;37(11):795-803; Proc Natl Acad Sci U S A. 2014 Jul 1;111(26):9651-6.
273.08
Formula
C9H9BrN2O3
CAS No.
188011-69-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (197.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424069
| In Vitro |
In vitro activity: Bikinin directly targets BIN2 of Arabidopsis GSK-3s and activates brassinosteroid-dependent gene expression. Bikinin also inhibits RD26 expression, and inhibits the induction of GUS activity by 150 mM NaCl in the RD26pro:GUS line. Kinase Assay: IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, compounds are tested in different concentrations diluted in assay buffer containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. Four microlitres of diluted compounds are added to 25 μM pGS-2 peptide substrate, 20 ng recombinant GSK-3β and 1 μM ATP to a total assay volume of 40 μl. The enzymatic reaction is stopped after 30 min of incubation at 30 °C by adding 40 μl KinaseGlo. The luminometric signal is allowed to stabilise for 10 min and the measured with a Glomax® 96 Microplate Luminometer. 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. |
|---|---|
| In Vivo | Bikinin strongly inhibits abscisic acid signaling outputs, and inhibits T180 phosphorylation of SnRK2.3 and its kinase activity in vivo. |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cells. 2014 Nov;37(11):795-803; Proc Natl Acad Sci U S A. 2014 Jul 1;111(26):9651-6. |
