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Lavendustin C

Cat. No. M28067
Lavendustin C Structure
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Biological Activity

Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+) kinase (IC50=0.5 µM) .

Chemical Information
Molecular Weight 275.26
Formula C14H13NO5
CAS Number 125697-93-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] A Nynca, et al. Domest Anim Endocrinol. Effects of the phytoestrogen, genistein, and protein tyrosine kinase inhibitor-dependent mechanisms on steroidogenesis and estrogen receptor expression in porcine granulosa cells of medium follicles

[2] Jieun Yoon, et al. Bioorg Med Chem Lett. A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly

[3] Riccardo Zucchi, et al. FASEB J. Ca2+ channel remodeling in perfused heart: Effects of mechanical work and interventions affecting Ca2+ cycling on sarcolemmal and sarcoplasmic reticulum Ca2+ channels

[4] M Imoto, et al. Biochim Biophys Acta. Involvement of tyrosine kinase in growth factor-induced phospholipase C activation in NIH3T3 cells

[5] W K Agbotounou, et al. Eur J Pharmacol. Inhibition by two lavendustins of the tyrosine kinase activity of pp60F527 in vitro and in intact cells

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Keywords: Lavendustin C supplier, CaMK, inhibitors, activators

 
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