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PDI inhibitor 16F16

Cat. No. M8206
PDI inhibitor 16F16 Structure
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Biological Activity

16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.

Chemical Information
Molecular Weight 320.77
Formula C16H17ClN2O3
CAS Number 922507-80-0
Solubility (25°C) DMSO: 12 mg/mL
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] Dennis zcelik. Treatment of Neuroblastoma Cells with Inhibitors of Protein Disulfide Isomerase Upregulates NQO1 Activity

[2] Lin Li, et al. Design, synthesis and evaluation of protein disulfide isomerase inhibitors with nitric oxide releasing activity

[3] Yunjeong Kim, et al. Protein disulfide isomerases as potential therapeutic targets for influenza A and B viruses

[4] Celia K Foster, et al. Challenges in the evaluation of thiol-reactive inhibitors of human protein disulfide Isomerase

[5] Rose M Langsjoen, et al. Host oxidative folding pathways offer novel anti-chikungunya virus drug targets with broad spectrum potential

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