CAS NO: | 1401223-22-0 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Cas No. | 1401223-22-0 |
化学名 | N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide |
Canonical SMILES | CCCC1=CC=C(OCC(N(C(C)C)CC2=NC(C3=CN=CC=C3)=NO2)=O)C=C1 |
分子式 | C22H26N4O3 |
分子量 | 394.47 |
溶解度 | ≥ 70.7mg/mL in DMSO |
储存条件 | Desiccate at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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]. References: |