[CAS NO. 1401223-22-0] PI-1840
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PRODUCTS SPECIFICATIONS [1401223-22-0]
Store
Catalog
SLK-S7462
Brand
Selleck
CAS
1401223-22-0
DESCRIPTION [1401223-22-0]
Overview
| MDL | MFCD28142700 |
|---|---|
| Molecular Weight | 394.47 |
| Molecular Formula | C22H26N4O3 |
| SMILES | O=C(N(C(C)C)CC1=NC(C2=CC=CN=C2)=NO1)COC3=CC=C(CCC)C=C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL |
Description
PI-1840 is a reversible and selective inhibitor with 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).
Targets
| Chymotrypsin-like proteasome [1] |
| 27 nM |
In vitro
PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human MDA-MB-468 cells. In intact cancer cells, PI-1840 inhibits CT-L activity, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis.
In vivo
PI-1840 (150 mg/kg i.p.) inhibits the tumor growth in mice of MDA-MB-231 breast tumors.
References
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