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CAS No. : 133407-82-6
MCE 國(guó)際站:MG-132
產(chǎn)品活性:MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的,,可逆的蛋白酶體 (proteasome) 抑制劑,,IC50 為 100 nM,。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛,,是自噬 (autophagy) 激活劑,。MG-132 還誘導(dǎo)凋亡 (apoptosis)。
研究領(lǐng)域:Metabolic Enzyme/Protease | Autophagy | Apoptosis
作用靶點(diǎn):Proteasome | Autophagy | Apoptosis
In Vitro: MG-132 (Z-Leu-Leu-Leu-al) initiates neurite outgrowth in PC12 cells at a low concentration (30 nM) and is a very strong inhibitor of 20S proteasome.
MG-132 (10 μM; 1 hour) reverses the effects of TNF- α on I κ B degradation and NF-κ B activation in A549 cells.
MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition.
MG-132 (10-40 μM; 24 hours) significantly reduces the viability of C6 glioma cells in both time- and concentration-dependent manners and shows the IC50 of 18.5 μM at 24 hours.
MG-132 (18.5 μM; 24 hours) induces down-regulation of anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3.
In Vivo: MG132 (10 mg/kg; i.p.; daily for 25 days starting 5 days after EC9706 cells injection) significantly inhibits tumor growth of the EC9706 xenograft without causing toxicity to mice.
MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors.
MG-132 (1-10 μg/kg/24 hours; subcutaneously implanted osmotic pumps; for 8 days) greatly increases the expression levels of β-dystroglycan, α-dystroglycan, α-sarcoglycan, and dystrophin in skeletal muscle lysates in mice (six-month-old male C57BL/10ScSn DMD mdx mice).
相關(guān)產(chǎn)品:Bioactive Compound Library Plus | Tamoxifen | Doxorubicin hydrochloride | Bafilomycin A1 | Y-27632 | 2-Deoxy-D-glucose | Paclitaxel | Angiotensin II human | Z-VAD-FMK | Acetylcysteine | LY294002 | Actinomycin D | SB-431542 | Staurosporine | 5-Fluorouracil | Oxaliplatin | Bortezomib | Sorafenib | Trametinib | Etoposide | Gemcitabine | Temozolomide | Monomethyl auristatin E | Mdivi-1 | Rotenone | Deferoxamine mesylate | Decitabine | CCCP | Metformin | Ruxolitinib | DAPT
熱門產(chǎn)品線:重組蛋白 | 藥物篩選 | 天然產(chǎn)物 | 熒光染料 | PROTAC | 同位素標(biāo)記物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
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