PI-1840
- CAS No.
- 1401223-22-0
- Chemical Name:
- PI-1840
- Synonyms
- PI-1840;CS-2559;PI 1840;PI1840;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;Acetamide, N-(1-methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-;cell proliferation,Proteasome,Caspase,proteasome substrates,poly ADP ribose polymerase,inhibit,NF-κB,Autophagy,cell cycle,anticancer,PI-1840,Apoptosis,Bcl-2 Family,MG-63 cells,Nuclear factor-kappaB,Inhibitor,U2-OS cells,PARP,PI1840,Nuclear factor-κB
- CBNumber:
- CB32716337
- Molecular Formula:
- C22H26N4O3
- Molecular Weight:
- 394.47
- MDL Number:
- MFCD28142700
- MOL File:
- 1401223-22-0.mol
- MSDS File:
- SDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H317-H319 |
| Precautionary statements | P280-P305+P351+P338 |
PI-1840 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | P400040 | PI1840 | 1401223-22-0 | 250mg | $2420 | 2021-12-16 | Buy |
| Medical Isotopes, Inc. | 61270 | PI1840 | 1401223-22-0 | 250mg | $3200 | 2021-12-16 | Buy |
| AK Scientific | 2655AH | N-Isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide | 1401223-22-0 | 5g | $8555 | 2021-12-16 | Buy |
| AK Scientific | 2655AH | N-Isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide | 1401223-22-0 | 10g | $11387 | 2021-12-16 | Buy |
| Medical Isotopes, Inc. | 61270 | PI1840 | 1401223-22-0 | 10mg | $650 | 2021-12-16 | Buy |
PI-1840 Chemical Properties,Uses,Production
Uses
PI 1840 is a novel rapidly reversible proteasome inhibitor with antitumor activity.
Biological Activity
pi-1840 is a potent and selective inhibitor of proteasome with ic50 value of 27 nm for chymotrypsinlike (ct-l) activity [1].the 26s proteasome consists of a 19s regulatory particle (rp) and a 20s core particle. the 26s proteasome have three main catalytic activities: chymotrypsin-like (ct-l), peptidylglutamyl peptide hydrolyzing-like (pgph-l) and trypsin-like (t-l) activities. ct-l activity plays an important role in the degradation of tumor suppressor and apoptotic proteins [1].pi-1840 is a rapidly reversible and non-covalent proteasome ct-l inhibitor. pi-1840 exhibited excellent selectivity for ct-l over pgph-l and t-l activities. in mda-mb-468 human breast cancer cells, pi-1840 inhibited the ct-l activity with ic50 value of 0.37 μm and inhibited cell survival/proliferation [1]. also, pi-1840 exhibited 121-fold selectivity for the constitutive 20 s proteasome over the immunoproteasome with ic50 values of 18 and 2170 nm, respectively. in mda-mb-468 cells, pi-1840 caused the accumulation of ct-l substrates iκb-α, p27 and bax. also, pi-1840 reduced the levels of survivin, p-akt and ser(p)-6 and induced apoptosis through poly(adp-ribose) polymerase cleavage and caspase-3 activation [2].in nude mice bearing human breast tumor, pi-1840 (150 mg/kg/day, i.p, daily) inhibited tumor growth by 85% [2].
Enzyme inhibitor
This potent proteasome inhibitor (FW = 394.38 g/mol) selectively targets its chymotrypsin-like activity, or CT-L (IC50 = 27 nM), while showing much weaker action (IC50 values >100 μM) against its Trypsin-Like (T-L) and peptidylglutamyl peptide hydrolyzing, or PGPH activities. Mass spectrometry and equilibrium dialysis show no evidence of covalent linkage of PI-1840 with any proteasomal protein component. In intact cancer cells, PI-1840 inhibits CT-L activity, inducing the accumulation of proteasome substrates p27, Bax and IκB-α, thereby inhibiting survival pathways and viability, and inducing apoptosis. PI=1840 is also >100x more active against the constitutive proteasome, compared to immunoproteasome.
target
CT-L
References
[1]. ozcan s, kazi a, marsilio f, et al. oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. j med chem, 2013, 56(10): 3783-3805.
[2]. kazi a, ozcan s, tecleab a, et al. discovery of pi-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. j biol chem, 2014, 289(17): 11906-11915.
PI-1840 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hi-Tech Chemistry Corp | 0519-86626038 | yuhh@hitechem.com | CHINA | 811 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 6011 | 61 |
| HuiFeiChem(WuXi) PharmaTech Co.,Ltd | 0510-0510-83593305 | sales@huifeichem.com | China | 104 | 62 |