PI-1840 |
| Catalog No.GC15802 |
PI-1840은 IC50 값이 27nM인 강력하고 선택적 키모트립신 유사(CT-L) 억제제입니다. PI-1840은 G2/M기에서 세포 증식을 억제하고 세포 주기를 정지시킵니다. PI-1840은 세포사멸을 유도하고 자가포식을 유도합니다. PI-1840은 프로테아좀 기질 p27, Bax 및 IκB-α의 축적을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1401223-22-0
Sample solution is provided at 25 µL, 10mM.
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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:
[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.
| Cas No. | 1401223-22-0 | SDF | |
| Chemical Name | 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 | ||
| Formula | C22H26N4O3 | M.Wt | 394.47 |
| Solubility | ≥ 70.7mg/mL in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.535 mL | 12.6752 mL | 25.3505 mL |
| 5 mM | 0.507 mL | 2.535 mL | 5.0701 mL |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.535 mL |
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μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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