5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
|Solubility (25°C)||DMSO 39 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Krystal M Butler-Fernndez, et al. Molecules. Synthesis, Anti-Cancer and Anti-Migratory Evaluation of 3,6-Dibromocarbazole and 5-Bromoindole Derivatives
 Malose J Mphahlele, et al. Pharmaceuticals (Basel). Synthesis, Evaluation of Cytotoxicity and Molecular Docking Studies of the 7-Acetamido Substituted 2-Aryl-5-bromo-3-trifluoroacetylindoles as Potential Inhibitors of Tubulin Polymerization
 J Tupper, et al. Cancer Gene Ther. In vivo characterization of horseradish peroxidase with indole-3-acetic acid and 5-bromoindole-3-acetic acid for gene therapy of cancer
 Oscar R Surez-Castillo, et al. J Nat Prod. Synthesis of bromoindole alkaloids from Laurencia brongniartii
 Deniz Tasdemir, et al. Z Naturforsch C J Biosci. Cytotoxic bromoindole derivatives and terpenes from the Philippine marine sponge Smenospongia sp
|Related GSK-3 Products|
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 a potent AhR (aryl hydrocarbon receptor) agonist.
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 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.
WAY-333184 is a inhibitor of glycogen synthase kinase-3b (GSK-3b).
WAY-333175 is a inhibitor of glycogen synthase kinase-3b (GSK-3b).
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