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Chemical Structure : PI-1840
CAS No.: 1401223-22-0
Catalog No.: PC-42948Not For Human Use, Lab Use Only.
PI-1840 is a potent, selective, noncovalent, reversible inhibitor for proteasome chymotrypsin-like (CT-L) activity with IC50 of 27 nM, shows no effect on trypsin-like and peptidylglutamyl peptide hydrolyzing activities (IC50>100 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote |
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PI-1840 is a potent, selective, noncovalent, reversible inhibitor for proteasome chymotrypsin-like (CT-L) activity with IC50 of 27 nM, shows no effect on trypsin-like and peptidylglutamyl peptide hydrolyzing activities (IC50>100 uM).
PI-1840 also displays 100-fold more selectivity for the constitutive proteasome over the immunoproteasome.
PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis in intact cancer cells, also sensitizes human cancer cells to the mdm2/p53 disruptor Nutlin.
PI-1840 suppresses the growth in nude mice of human breast tumor xenografts.
| M.Wt | 394.4668 | |
| Formula | C22H26N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Acetamide, N-(1-methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]- |
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1. Kazi A, et al. J Biol Chem. 2014 Apr 25;289(17):11906-15.
2. Ozcan S, et al. J Med Chem. 2013 May 23;56(10):3783-805.
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