Bikinin is a strong activator of brassinosteroid (BR) signaling. It is an Arabidopsis GSK-3 Inhibitor, an Arabidopsis SHAGGY-related Kinase Inhibitor, and a GSK-3-like Kinase BIN2 Inhibitor. Bikinin directly inhibits BIN2 (group II GSK3s) by interfering with ATP binding. Bikinin is specific toward a subset of Arabidopsis GSK3 kinases including BIN2 and ASK α, γ, ε, ι, and θ.
| Molecular Weight | 273.08 |
| Formula | C9H9BrN2O3 |
| CAS Number | 188011-69-0 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Wilfried Rozhon, et al. Inhibitors of Brassinosteroid Biosynthesis and Signal Transduction
[2] Takema Sasaki, et al. Imaging of Developing Metaxylem Vessel Elements in Cultured Hypocotyls
| Related GSK-3 Products |
|---|
| 6-Me-ATP
6-Me-ATP (N6-Methyl-ATP) is a N6-modified ATP derivative. |
| PROTAC GSK-3β Degrader-1
PROTAC GSK-3β Degrader-1 is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. |
| GSK-3β inhibitor 13
GSK-3β inhibitor 13 is an orally active and potent GSK-3β inhibitor with blood-brain permeability. |
| GSK-3 inhibitor 3
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. |
| GSK-3 inhibitor 4
GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. |
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