| Bioactivity | PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α[1][2]. | ||||||||||||
| Invitro | PI-1840 (5-60 µM; 24 and 48 h) inhibits the proliferation of MG-63 and U2-OS cells[1].PI-1840 (40 µM (U2-OS cells) and 60 µM (MG-63 cells); 24 and 48 h) induces cell cycle arrest at the G2/M phase[1].PI-1840 (15-60 µM (MG-63 cells), 10-40 µM (U2-OS cells); 48 h) induces apoptosis through NF-κB pathway in MG-63 and U2-OS cells. PI-1840 induces autophagy in MG-63 and U2-OS cells[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | PI-1840 (150 mg/kg; i.p.; daily, for 14 d) inhibits the growth of human breast tumor xenografts in nude mice[2]. Animal Model: | ||||||||||||
| Name | PI-1840 | ||||||||||||
| CAS | 1401223-22-0 | ||||||||||||
| Formula | C22H26N4O3 | ||||||||||||
| Molar Mass | 394.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kazi A, 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):11906-11915. [2]. Chen Y, et, al. Non covalent proteasome inhibitor PI 1840 induces apoptosis and autophagy in osteosarcoma cells. Oncol Rep. 2019 May;41(5):2803-2817. |