1401223-22-0

1401223-22-0 - Names and Identifiers

Name	N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide
Synonyms	PI1840 PI-1840 CS-2559 PI 1840 N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide N-(1-methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-acetamide
CAS	1401223-22-0
EINECS	604-604-1

1401223-22-0 - Physico-chemical Properties

Molecular Formula	C22H26N4O3
Molar Mass	394.47
Solubility	Soluble in DMSO
Storage Condition	-20℃
Use	PI-1840 is a is a novel rapidly reversible proteasome inhibitor with antitumor activity. It shows selective inhibitor for chymotrypsin-like (CT-L) over trypsin-like and peptidylglutamyl peptide hydrolyzing activities of the proteasome.
In vitro study	PI-1840 potently inhibits the activity of leucosome MDA-MB-468 in intact human CT-L cancer cells and inhibits proliferation/survival of human MDA-MB-468 cells. In intact cancer cells, PI-1840 inhibits CT-L of activity, induces accumulation of the proteasome substrates p27,Bax, and IKB-α, inhibits survival pathways and viability, and induces apoptosis.
In vivo study	PI-1840 (150 mg/kg, I. P.) inhibited tumor growth in MDA-MB-231 breast tumor-bearing mice.

1401223-22-0 - Reference

Reference

1: Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014;289(17):11906-11915. doi:10.1074/jbc.M113.533950.

1401223-22-0 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.535 ml	12.675 ml	25.351 ml
5 mM	0.507 ml	2.535 ml	5.07 ml
10 mM	0.254 ml	1.268 ml	2.535 ml
5 mM	0.051 ml	0.254 ml	0.507 ml

Last Update：2024-01-02 23:10:35

1401223-22-0 - Cell Experiment

Cells are plated in 96-well plates in 100 μL medium and allowed to attach overnight. Cells are then incubated for 120 h with varying concentrations of inhibitors. Media is aspirated and replaced with 100 μL complete media containing 1 mg/ml MTT and incubated for three hours at 37 °C in 5% CO2 humidified incubator. Media is then aspirated and DMSO is added. Cells are incubated for 10 min at room temperature while shaking, and the absorbance is determined at 540 nm using a μQuant spectrophotometric plate reader. The IC50 values are determined using equation under CT-L, T-L, PGPH-L proteolytic activity assays.(Only for Reference) Cell lines: MDA-MB-468 cells

Last Update：2023-08-16 21:32:38

1401223-22-0 - Reference Information

biological activity	PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM, which has no effect on the proteolytic activities of the other two main proteasomes (trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L)).
in vitro study	PI-1840 effectively inhibits the activity of albase CT-L in intact human MDA-MB-468 cancer cells and inhibits the proliferation/survival of human MDA-MB-468 cells. In intact cancer cells, PI-1840 inhibits CT-L activity, induces accumulation of proteasome substrates p27,Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis.
in vivo study	PI-1840 (150 mg/kg, intraperitoneal injection) inhibits tumor growth in mice with MDA-MB-231 breast tumors.

Last Update：2024-04-09 20:49:11