Structure of (R)-MG-132
CAS No.: 1211877-36-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
(R)-MG132 can act as an inhibitor of proteasome and be used in ubiquitination assay.
Synonyms: (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al; MG132
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 1211877-36-9 |
Formula : | C26H41N3O5 |
M.W : | 475.62 |
SMILES Code : | [C@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)CC(C)C)=O)(C(N[C@@H](CC(C)C)C=O)=O)CC(C)C |
Synonyms : |
(S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al; MG132
|
MDL No. : | MFCD28580122 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
Target |
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
mouse brain synaptosomes | 10 µM | 30 min | To investigate the effects of proteasome inhibition on presynaptic architecture and function, results showed that MG132 treatment significantly reversed the structural defects in RIM1α KO synapses and restored release probability to WT levels. | PMC3664715 |
HEI-193 schwannoma cells | 2.5 μM | 24, 48, 72 h | To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the proliferation of schwannoma cells. Results showed that MG-132 enhanced the inhibitory effect of Nutlin-3 on cell proliferation. | PMC6197711 |
RT4-D6P2T schwannoma cells | 2.5 μM | 24, 48, 72 h | To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the proliferation of schwannoma cells. Results showed that MG-132 enhanced the inhibitory effect of Nutlin-3 on cell proliferation and narrowed the sensitivity differences between cells with different merlin expression status. | PMC6197711 |
Naïve CD4+ T cells | 10 µM | 2 h | Promote CD69+ iTregs differentiation | PMC10091886 |
RVSMCs | 10 μM | 6 days | Treatment with MG132 or lactacystin halved Pi-induced calcium deposition, demonstrating proteasome inhibition alleviates vascular calcification | PMC4740400 |
A10 cells (RVSMC line) | 10 μM | 4 h | MG132 treatment enhanced HDAC1 ubiquitination under Pi stimulation, confirming HDAC1 degradation via the proteasomal pathway | PMC4740400 |
rat vascular smooth muscle cells (RVSMCs) | 10 μM | 4 h | MG132 markedly attenuated Pi-induced HDAC1 reduction, indicating proteasomal inhibition prevents HDAC1 degradation | PMC4740400 |
Plasmodium falciparum 3D7 parasite-infected red blood cells | 100 nM | 72 h | Inhibition of 26S proteasome activity significantly inhibited α-spectrin degradation and parasite proliferation | PMC11005373 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
BALB/c nude mice | RT4-D6P2T and HEI-193 schwannoma xenograft models | Intraperitoneal injection | 5 mg/kg | Once daily for 14 days | To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the growth of schwannoma xenografts. Results showed that the combined treatment significantly inhibited tumor growth and induced apoptosis of tumor cells. | PMC6197711 |
Mice | DSS-induced colitis model | Intraperitoneal injection | 15 μM/kg | 9 days | Promote CD69+ Tregs differentiation but fail to effectively alleviate colitis | PMC10091886 |
Mice | VD3-induced vascular calcification model | Intraperitoneal injection | 2.5 mg/kg | Daily administration for 9 days | MG132 significantly reduced VD3-induced aortic calcium deposition and prevented HDAC1 downregulation | PMC4740400 |
Mouse | P23H mice | Intraperitoneal injection | 5 mg/kg | Single injection | To enhance the detection of ubiquitinated proteins | PMC6639359 |
C57BL/6 mice | Plasmodium berghei ANKA infection model | Intraperitoneal injection | 1.5 mg/kg | Once daily for 9 days | Inhibition of 26S proteasome activity significantly reduced parasitemia | PMC11005373 |
Mice | Vitamin D receptor knockout mice | Intraperitoneal injection | 2.5 mg/kg | Once daily for 2 days | To assess protein ubiquitination levels, results showed higher total ubiquitination and K48-linked ubiquitination in skeletal muscles of vdr /C0//C0 mice. | PMC8818613 |
Mice | Healthy mice | Intraperitoneal injection | 10 μg/kg | Single injection, samples collected after 24 hours | MG-132, as a proteasome inhibitor, was used to study the effect of agmatine on β-catenin stability. Results showed that agmatine increased β-catenin stability by suppressing Rnf128-mediated ubiquitination degradation. | PMC11086030 |
Mice | Wildtype mice | Intraperitoneal injection | 50µg/g | Single injection, analyzed after 3 hours | MG132 significantly increased VEGF receptor levels in type H vessel columns | PMC5580829 |
Tags: R-MG-132 | MG-132(R) | stereoisomer | chymotrypsin-like activity | 26S proteasome | apoptosis | ubiquitinated proteins | 1211877-36-9
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