PI-1840

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Chemical Structure| 1401223-22-0 同义名 : -
CAS号 : 1401223-22-0
货号 : A716849
分子式 : C22H26N4O3
纯度 : 98%
分子量 : 394.47
MDL号 : MFCD28142700
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(266.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • 20S proteasome

    Chymotrypsin-like proteasome, IC50:27 nM
描述 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
参考文献

[1]Ozcan S, Kazi A, Marsilio F, et al. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. J Med Chem. 2013 May 23;56(10):3783-805.

[2]Kazi A, Ozcan S, et al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Apr 25;289(17):11906-15.