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Bisindolylmaleimide V

Cat. No. M27835
Bisindolylmaleimide V Structure
Synonym:

BIM V

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Biological Activity

Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 µM. Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 of 8 µM.

Chemical Information
Molecular Weight 341.36
Formula C21H15N3O2
CAS Number 113963-68-1
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Aeran Kim, et al. Eur J Pharmacol. Direct block by bisindolylmaleimide of the voltage-dependent K+ currents of rat mesenteric arterial smooth muscle

[2] Sari Voutilainen-Myllylä, et al. Eur J Pharmacol. Chelerythrine and bisindolylmaleimide I prolong cardiac action potentials by protein kinase C-independent mechanism

[3] Rei Asakai, et al. Neurosci Res. Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons

[4] I Hers, et al. FEBS Lett. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity

[5] S Lazareno, et al. Eur J Pharmacol. Muscarinic interactions of bisindolylmaleimide analogues

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Keywords: Bisindolylmaleimide V, BIM V supplier, S6 Kinase, inhibitors, activators

 
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