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Formula | C26H41N3O5 |
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Molecular Weight | 475.62 | CAS No. | 1211877-36-9 | ||||
Solubility (25°C)* | In vitro | DMSO | 95 mg/mL (199.73 mM) | ||||
Ethanol | 95 mg/mL (199.73 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) is a potent proteasome (ChTL, TL, and PGPH) inhibitor. MG132 also inhibits calpain (IC50=1.2 μM). MG132 can be used to induce animal models of Parkinson’s disease. | ||
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In vitro | MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal. [1] MG-132 (10 μM) potently inhibits TNF-α-induced NF-κB activation, interleukin-8 (IL-8) gene transcription, and IL-8 protein release in A549 cells by inhibition of proteasome-mediated IκBα degradation. [2] MG-132 treatment potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition. [3] Unlike BzLLLCOCHO or PS-341, MG-132 treatment results in weak inhibition of the chymotrypsinlike (CT-L) and peptidylglutamyl peptide hydrolysing (PGPH) activities of the 26S proteasome, whereas multiple myeloma cells (U266 and OPM-2) are more sensitive to induction of apoptosis by MG-132 than BzLLLCOCHO. [4] MG-132 (1 μM) sensitizes TRAIL-resistant prostate cancer cells by activating the AP-1 family members c-Fos and c-Jun, which, in turn, repress the antiapoptotic molecule c-FLIP(L). [5] MG-132 significantly enhances the ability of inositol hexakisphosphate (IP6) to reduce cellular metabolic activity in both PC3 and DU145 androgen-independent prostate cancer (AIPCa) cell lines. [6] |
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In vivo | Administration of MG-132 effectively rescues the expression levels and plasma membrane localization of dystrophin, β-dystroglycan, α-bdystroglycan, and α-sarcoglycan in skeletal muscle fibers from mdx mice, reduces muscle membrane damage, and ameliorates the histopathological signs of muscular dystrophy. [7] MG-132 treatment significantly reduces immobilization-induced skeletal muscle atrophy in mice, by downregulating the muscle-specific ubiquitin ligases atrogin-1/MAFbx and MuRF-1 mRNA. [8] |
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Data from [Data independently produced by Nat Cell Biol, 2015, 17(1), 95-103]
Data from [Data independently produced by Cell Rep, 2015, 11(9), 1458-73]
Data from [Data independently produced by Toxicol Appl Pharmacol, 2015, 286(2), 135-41]
Data from [Nucleic Acids Res, 2014, 42(1), 458-74]
Suppression of ITPKB degradation by Trim25 confers TMZ resistance in glioblastoma through ROS homeostasis [ Signal Transduct Target Ther, 2024, 9(1):58] | PubMed: 38438346 |
Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer [ Signal Transduct Target Ther, 2024, 9(1):65] | PubMed: 38461173 |
Trametinib sensitizes KRAS-mutant lung adenocarcinoma tumors to PD-1/PD-L1 axis blockade via Id1 downregulation [ Mol Cancer, 2024, 23(1):78] | PubMed: 38643157 |
Combined targeting of GPX4 and BCR-ABL tyrosine kinase selectively compromises BCR-ABL+ leukemia stem cells [ Mol Cancer, 2024, 23(1):240] | PubMed: 39465372 |
LINC00115 promotes chemoresistant breast cancer stem-like cell stemness and metastasis through SETDB1/PLK3/HIF1α signaling [ Mol Cancer, 2024, 23(1):60] | PubMed: 38520019 |
Trametinib sensitizes KRAS-mutant lung adenocarcinoma tumors to PD-1/PD-L1 axis blockade via Id1 downregulation [ Mol Cancer, 2024, 23(1):78] | PubMed: 38643157 |
Targeting a chemo-induced adaptive signaling circuit confers therapeutic vulnerabilities in pancreatic cancer [ Cell Discov, 2024, 10(1):109] | PubMed: 39468013 |
Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury [ Cell Metab, 2024, S1550-4131(24)00371-1] | PubMed: 39389061 |
Oncogenic fatty acid oxidation senses circadian disruption in sleep-deficiency-enhanced tumorigenesis [ Cell Metab, 2024, 36(7):1598-1618.e11] | PubMed: 38772364 |
Methylation of GPRC5A promotes liver metastasis and docetaxel resistance through activating mTOR signaling pathway in triple negative breast cancer [ Drug Resist Updat, 2024, 73:101063] | PubMed: 38335844 |
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