參考價	￥ 350

信號通路

MedChemExpress (M

CAS	133407-82-6	純度	99.97%
分子量	475.62	分子式	C??H??N?O?
供貨周期	現貨	規格	5 mg
貨號	HY-13259	應用領域	醫療衛生,化工,生物產業,制藥

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 還誘導凋亡 (apoptosis)。

詳細介紹

MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務。

MG-132

CAS No. : 133407-82-6

MCE 國際站：MG-132

產品活性：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 還誘導凋亡 (apoptosis)。

研究領域：Metabolic Enzyme/Protease | Autophagy | Apoptosis

作用靶點：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).