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PI-1840

Cat. No. M20599
PI-1840 Structure
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Biological Activity

PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

Chemical Information
Molecular Weight 394.47
Formula C22H26N4O3
CAS Number 1401223-22-0
Solubility (25°C) DMSO 78 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] Yajun Yang, et al. Bioorg Med Chem Lett. Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors

[2] Yuxi Chen, et al. Oncol Rep. Non‑covalent proteasome inhibitor PI‑1840 induces apoptosis and autophagy in osteosarcoma cells

[3] Jianjun Yu, et al. Eur J Med Chem. Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors

[4] Aslamuzzaman Kazi, et al. J Biol Chem. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity

[5] Sevil Ozcan, et al. J Med Chem. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors

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Keywords: PI-1840 supplier, Proteasome, inhibitors, activators

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