PI 1840
Modify Date: 2024-01-02 14:30:39
PI 1840 structure
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Common Name | PI 1840 | ||
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| CAS Number | 1401223-22-0 | Molecular Weight | 394.46700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H26N4O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PI 1840PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome. IC50 value: 27 nM(CT-L activities of the proteasome) [1]Target: CT-L inhibitorin vitro: PI-1840 is over 100-fold more selective for the constitutive proteasome over the immunoproteasome. Mass spectrometry and dialysis studies demonstrate that PI-1840 is a noncovalent and rapidly reversible CT-L inhibitor. 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. Furthermore, PI-1840 sensitizes human cancer cells to the mdm2/p53 disruptor, nutlin, and to the pan-Bcl-2 antagonist BH3-M6 [1].in vivo: PI-1840 but not bortezomib suppresses the growth in nude mice of human breast tumor xenografts [1]. |
| Name | N-isopropyl-2-(4-propylphenoxy)-N-(((3-pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide |
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| Synonym | More Synonyms |
| Description | PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome. IC50 value: 27 nM(CT-L activities of the proteasome) [1]Target: CT-L inhibitorin vitro: PI-1840 is over 100-fold more selective for the constitutive proteasome over the immunoproteasome. Mass spectrometry and dialysis studies demonstrate that PI-1840 is a noncovalent and rapidly reversible CT-L inhibitor. 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. Furthermore, PI-1840 sensitizes human cancer cells to the mdm2/p53 disruptor, nutlin, and to the pan-Bcl-2 antagonist BH3-M6 [1].in vivo: PI-1840 but not bortezomib suppresses the growth in nude mice of human breast tumor xenografts [1]. |
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| Related Catalog | |
| References |
| Molecular Formula | C22H26N4O3 |
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| Molecular Weight | 394.46700 |
| Exact Mass | 394.20000 |
| PSA | 81.35000 |
| LogP | 3.90010 |
| Storage condition | -20℃ |
| PI-1840 |