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Bortezomib
CAS No. : 179324-69-7
MCE 国际站：Bortezomib
产品活性：Bortezomib (PS-341) 是一种可逆性和选择性的蛋白酶体 (proteasome) 抑制剂，通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一种蛋白酶体抑制剂，具有抗癌活性。
研究领域：Metabolic Enzyme/Protease | NF-κB | Apoptosis | Autophagy
作用靶点：Proteasome | NF-κB | Apoptosis | Autophagy
In Vitro: Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.
Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines.
Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines.
The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells.
Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3).
In Vivo: Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice.
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