Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
生物活性
Discription
MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).
Targets
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Cell Research
Cell Line
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Description
References
In Vitro
Proteasome inhibition: MG-132 is a highly potent proteasome inhibitor, showing over 1000-fold greater activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of the 20S proteasome, with an IC50 of 100 nM compared to 110 μM. This potency extends to other proteasome-mediated processes, such as protein degradation and signaling regulation【1】.
Calpain inhibition: In addition to proteasome inhibition, MG-132 also inhibits calpain with an IC50 of 1.2 μM, indicating its dual capability in targeting both proteasomal and calpain-mediated pathways【1】.
Induction of neurite outgrowth: MG-132 promotes neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, demonstrating approximately 500 times higher potency compared to ZLLal. This highlights its potential applications in neuroregenerative research【1】.
Suppression of NF-κB activation: At 10 μM, MG-132 effectively blocks TNF-α-induced NF-κB activation in A549 cells by preventing proteasome-mediated degradation of IκBα. This also leads to significant inhibition of interleukin-8 (IL-8) gene transcription and protein release, showcasing its anti-inflammatory properties【2】.
p53-dependent apoptosis induction: MG-132 induces p53-dependent apoptosis in KIM-2 cells through the inhibition of the 26S proteasome, emphasizing its role in triggering apoptosis in cancer cells【3】.
Selective apoptotic activity in multiple myeloma: MG-132 exhibits distinct apoptotic effects on multiple myeloma cells (U266 and OPM-2), demonstrating higher sensitivity compared to other proteasome inhibitors like BzLLLCOCHO or PS-341. However, it shows relatively weaker inhibition of the chymotrypsin-like (CT-L) and peptidylglutamyl peptide hydrolyzing (PGPH) activities of the 26S proteasome【4】.
Sensitization of resistant cancer cells: At 1 μM, MG-132 sensitizes TRAIL-resistant prostate cancer cells by activating AP-1 transcription factors such as c-Fos and c-Jun, which suppress the anti-apoptotic protein c-FLIP(L), leading to enhanced apoptosis【5】.
Synergistic effects with other agents: MG-132 significantly enhances the anti-cancer effects of inositol hexakisphosphate (IP6) in androgen-independent prostate cancer cell lines (PC3 and DU145) by reducing cellular metabolic activity. This demonstrates its potential for combination therapies in resistant cancer types【6】.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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