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Bisindolylmaleimide VIII acetate

Cat. No. M31206
Bisindolylmaleimide VIII acetate Structure
Synonym:

Ro 31-7549 acetate; Bis VIII acetate

Size Price Availability Quantity
5mg USD 190  USD190 In stock
10mg USD 290  USD290 In stock
25mg USD 620  USD620 In stock
50mg USD 980  USD980 In stock
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Quality Control & Documentation
Biological Activity

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate (5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners.

Chemical Information
Molecular Weight 458.51
Formula C26H26N4O4
CAS Number 138516-31-1
Form Solid
Solubility (25°C) DMSO >100 mg/mL (Need ultrasonic)
Storage -20°C, dry, sealed
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] Akeem O Lawal, et al. Environ Toxicol Pharmacol. Nrf2-mediated adaptive response to cadmium-induced toxicity involves protein kinase C delta in human 1321N1 astrocytoma cells

[2] Zuzana Bacová, et al. Cell Physiol Biochem. Different signaling pathways involved in glucose- and cell swelling-induced insulin secretion by rat pancreatic islets in vitro

[3] Todd M Kolb, et al. Toxicol Sci. The tumor promoter 12-O-tetradecanoylphorbol 13-acetate (TPA) provokes a prolonged morphologic response and ERK activation in Tsc2-null renal tumor cells

[4] N A Turner, et al. Biochem Soc Trans. Protein kinase C subtypes associated with the regulation of noradrenaline release in human SH-SY5Y neuroblastoma cells

[5] P Germano, et al. J Biol Chem. Phosphorylation of the gamma chain of the high affinity receptor for immunoglobulin E by receptor-associated protein kinase C-delta

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Keywords: Bisindolylmaleimide VIII acetate, Ro 31-7549 acetate; Bis VIII acetate supplier, PKC, inhibitors, activators

 
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