MeBIO, an analog of 6-bromoindirubin-3'-oxime, has been suggested to possess the structural basis for a potent and selective inhibitor of glycogen synthase kinase-3 (GSK3) and cyclin-dependent kinases. MeBIO displays minimal activity against CDK1/Cyclin B, GSK-3, and CDK5/p25 (IC50 values are 92.0, 44-100 and >100 μM respectively). MeBIO is inactive on GSK-3β. MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist.
Molecular Weight | 370.20 |
Formula | C17H12BrN3O2 |
CAS Number | 667463-95-8 |
Solubility (25°C) | DMSO 10 mg/mL (May need warming and ultrasonic) |
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.
Related GSK-3 Products |
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Indirubin-3′-oxime
Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity. |
9-ing-41
9-ING-41 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with antitumor activity. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β. |
5-Bromoindole
5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). |
WAY-333184
WAY-333184 is a inhibitor of glycogen synthase kinase-3b (GSK-3b). |
WAY-333175
WAY-333175 is a inhibitor of glycogen synthase kinase-3b (GSK-3b). |
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