(R)-MG132
(R)-MG132
CAS: 1211877-36-9
Molecular Formula: C26H41N3O5
(R)-MG132 - Names and Identifiers
(R)-MG132 - Physico-chemical Properties
| Molecular Formula | C26H41N3O5 |
| Molar Mass | 475.62 |
| Appearance | powder |
| Storage Condition | -20°C |
| Physical and Chemical Properties | Bioactive MG132 (Z-Leu-Leu-Leu-al) is a proteasome and calpain inhibitor with cell permeability, IC50 is 100 nM and 1.2 μM respectively. MG132 can activate autophagy and induce apoptosis of tumor cells. |
| In vitro study | MG-132 inhibition of 20S proteasome ZLLL-MCA degradation activity, IC50 100 nM, than ZLLal(IC50 110 μm) more than 1000 times. MG-132 also inhibited calpain with an IC50 of 1.2 μm. MG-132 induced neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, showing 500-fold greater potency than ZLLal. MG-132 (10 μm) effectively inhibits TNF-α-induced NF-κB activation and interleukin-8 (IL-8) gene transcription in A549 cells by inhibiting proteasome-mediated degradation of IκBα, and IL-8 protein release. MG-132 treatment effectively Induced p53-Dependent KIM-2 cell apoptosis by inhibiting the 26S proteasome. Unlike the BzLLLCOCHO or PS-341, the MG-132 treatment inhibited the chymin-like (CT-L) and peptide glutamyl peptide hydrolysis (PGPH) activity of the 26S proteasome weakly compared to the BzLLLCOCHO,MG-132 was able to more efficiently induce apoptosis in multiple myeloma cells (U266 and OPM-2). MG-132 (1 μm) sensitizes TRAIL-resistant prostate cancer cells by activating AP-1 family members c-Fos and c-Jun, which in turn inhibits the anti-apoptotic molecule c-FLIP(L). MG-132 the effect of inositol hexaphosphate (IP6) was significantly enhanced to reduce the cellular metabolic activity of PC3 and DU145 androgen independent prostate cancer (AIPCa) cell lines. |
| In vivo study | MG-132 administration effectively restores the expression levels and plasma membrane localization of dystrophin, β-dystrophin, α-dystrophin, and α-myoglycoprotein in skeletal muscle fibers of mdx mice, reduces muscle membrane damage and improves histopathological signals in muscular dystrophy. MG-132 treatment significantly reduced immobilization-induced skeletal muscle atrophy in mice by down-regulating muscle-specific ubiquitin ligase atrogin-1/MAFbx and MuRF-1 mRNA. |
(R)-MG132 - Risk and Safety
| WGK Germany | 3 |
(R)-MG132 - Uses and synthesis methods
Target
Target Value
Proteasome
(Cell-free assay) 100 nM
in vitro studies
MG-132 inhibits the degradation activity of 20S proteasome ZLLL-MCA. IC50 is 100 nM, which is more than 1000 times more effective than ZLLal(IC50 is 110 μM). MG-132 also inhibits calpain with an IC50 of 1.2 μM. MG-132 induced neurite proliferation in PC12 cells at an optimal concentration of 20 nM, showing a 500-fold higher potency than ZLLal. MG-132 (10 μM) effectively inhibits TNF-α-induced NF-& kappa in A549 cells by inhibiting proteasome-mediated I & kappa;B activation, interleukin -8 (IL-8) gene transcription, and IL-8 protein release. MG-132 treatment effectively induced apoptosis of p53-dependent KIM-2 cells by inhibiting 26S proteasome. Different from BzLLLCOCHO or PS-341,MG-132 treatment has weak inhibition on chylein-like (CT-L) and peptide glutamyl peptide hydrolysis (PGPH) activities of 26S proteasome, while MG-132 can more effectively induce apoptosis of multiple myeloma cells (U266 and OPM-2) than BzLLLCOCHO. MG-132 (1 μM) sensitizes TRAIL-resistant prostate cancer cells by activating c-Fos and c-Jun of AP-1 family members, which in turn inhibits anti-apoptotic molecular c-FLIP(L). MG-132 significantly enhanced the effect of inositol hexaphosphate (IP6) to reduce the cell metabolic activity of PC3 and DU145 androgen-independent prostate cancer (AIPCa) cell lines.
In vivo studies
MG-132 administration effectively restored the expression levels and plasma membrane localization of dystrophin, β-dystrophin, α-dystrophin, and α-dystrophin in skeletal muscle fibers of mdx mice, reduced muscle membrane damage, and improved histopathological signals of muscular dystrophy. MG-132 treatment significantly reduced skeletal muscle atrophy induced by immobilization in mice by down-regulating muscle-specific ubiquitin ligase atrogin-1/MAFbx and MuRF-1 mRNA.
Last Update：2024-04-09 22:09:11
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