Page last updated: 2024-12-08

mg 262

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Description

MG 262: a proteasome inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID490002
CHEMBL ID114388
SCHEMBL ID12384366
MeSH IDM0384451

Synonyms (23)

Synonym
[(1r)-1-[[(2s)-2-[[(2s)-2-(benzyloxycarbonylamino)-4-methyl-pentanoyl]amino]-4-methyl-pentanoyl]amino]-3-methyl-butyl]boronic acid
l-leucinamide, n-[(phenylmethoxy)carbonyl]-l-leucyl-n1-[(1r)-1-borono-3-methylbutyl]-
mg 262
mg-262
boro-lll
mg262
CHEMBL114388 ,
[(1r)-3-methyl-1-[[(2s)-4-methyl-2-[[(2s)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]pentanoyl]amino]butyl]boronic acid
bdbm50069984
(r)-1-((s)-2-((s)-2-(benzyloxycarbonyl)-4-methylpentanamido)-4-methylpentanamido)-3-methylbutylboronic acid
ps-iii
549v4dp94w ,
unii-549v4dp94w
l-leucinamide, n-((phenylmethoxy)carbonyl)-l-leucyl-n-(1-borono-3-methylbutyl)-, (r)-
l-leucinamide, n-((phenylmethoxy)carbonyl)-l-leucyl-n-((1r)-1-borono-3-methylbutyl)-
SCHEMBL12384366
DTXSID80170795
((5s,8s,11r)-5,8-diisobutyl-13-methyl-3,6,9-trioxo-1-phenyl-2-oxa-4,7,10-triazatetradecan-11-yl)boronic acid
Q27261199
STARBLD0016848
CS-0029134
HY-108551
AKOS040744960
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin BHomo sapiens (human)Ki0.00610.00001.21808.6000AID50483
Proteasome subunit beta type-1Homo sapiens (human)Ki48.00000.13001.56255.5200AID264537
Proteasome subunit beta type-5Homo sapiens (human)Ki0.00230.00060.01040.0700AID264535
Proteasome subunit beta type-2Homo sapiens (human)Ki110.00000.00102.34535.5200AID264536
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
proteolysisCathepsin BHomo sapiens (human)
thyroid hormone generationCathepsin BHomo sapiens (human)
collagen catabolic processCathepsin BHomo sapiens (human)
epithelial cell differentiationCathepsin BHomo sapiens (human)
regulation of apoptotic processCathepsin BHomo sapiens (human)
decidualizationCathepsin BHomo sapiens (human)
symbiont entry into host cellCathepsin BHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin BHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin BHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProteasome subunit beta type-1Homo sapiens (human)
proteolysis involved in protein catabolic processProteasome subunit beta type-1Homo sapiens (human)
proteolysisProteasome subunit beta type-5Homo sapiens (human)
response to oxidative stressProteasome subunit beta type-5Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProteasome subunit beta type-5Homo sapiens (human)
response to organonitrogen compoundProteasome subunit beta type-2Homo sapiens (human)
response to organic cyclic compoundProteasome subunit beta type-2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProteasome subunit beta type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin BHomo sapiens (human)
protein bindingCathepsin BHomo sapiens (human)
collagen bindingCathepsin BHomo sapiens (human)
peptidase activityCathepsin BHomo sapiens (human)
cysteine-type peptidase activityCathepsin BHomo sapiens (human)
proteoglycan bindingCathepsin BHomo sapiens (human)
protein bindingProteasome subunit beta type-1Homo sapiens (human)
threonine-type endopeptidase activityProteasome subunit beta type-5Homo sapiens (human)
protein bindingProteasome subunit beta type-5Homo sapiens (human)
peptidase activityProteasome subunit beta type-5Homo sapiens (human)
endopeptidase activityProteasome subunit beta type-5Homo sapiens (human)
protein bindingProteasome subunit beta type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular regionCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
external side of plasma membraneCathepsin BHomo sapiens (human)
apical plasma membraneCathepsin BHomo sapiens (human)
endolysosome lumenCathepsin BHomo sapiens (human)
melanosomeCathepsin BHomo sapiens (human)
perinuclear region of cytoplasmCathepsin BHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular exosomeCathepsin BHomo sapiens (human)
peptidase inhibitor complexCathepsin BHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
nucleusProteasome subunit beta type-1Homo sapiens (human)
cytoplasmProteasome subunit beta type-1Homo sapiens (human)
proteasome complexProteasome subunit beta type-1Homo sapiens (human)
extracellular regionProteasome subunit beta type-1Homo sapiens (human)
nucleusProteasome subunit beta type-1Homo sapiens (human)
nucleoplasmProteasome subunit beta type-1Homo sapiens (human)
cytosolProteasome subunit beta type-1Homo sapiens (human)
secretory granule lumenProteasome subunit beta type-1Homo sapiens (human)
extracellular exosomeProteasome subunit beta type-1Homo sapiens (human)
ficolin-1-rich granule lumenProteasome subunit beta type-1Homo sapiens (human)
proteasome core complexProteasome subunit beta type-1Homo sapiens (human)
proteasome core complex, beta-subunit complexProteasome subunit beta type-1Homo sapiens (human)
nucleusProteasome subunit beta type-5Homo sapiens (human)
cytoplasmProteasome subunit beta type-5Homo sapiens (human)
proteasome complexProteasome subunit beta type-5Homo sapiens (human)
nucleusProteasome subunit beta type-5Homo sapiens (human)
nucleoplasmProteasome subunit beta type-5Homo sapiens (human)
centrosomeProteasome subunit beta type-5Homo sapiens (human)
cytosolProteasome subunit beta type-5Homo sapiens (human)
extracellular exosomeProteasome subunit beta type-5Homo sapiens (human)
proteasome core complexProteasome subunit beta type-5Homo sapiens (human)
proteasome core complex, beta-subunit complexProteasome subunit beta type-5Homo sapiens (human)
cytosolProteasome subunit beta type-5Homo sapiens (human)
nucleusProteasome subunit beta type-2Homo sapiens (human)
cytoplasmProteasome subunit beta type-2Homo sapiens (human)
proteasome complexProteasome subunit beta type-2Homo sapiens (human)
nucleusProteasome subunit beta type-2Homo sapiens (human)
nucleoplasmProteasome subunit beta type-2Homo sapiens (human)
cytosolProteasome subunit beta type-2Homo sapiens (human)
membraneProteasome subunit beta type-2Homo sapiens (human)
extracellular exosomeProteasome subunit beta type-2Homo sapiens (human)
proteasome core complexProteasome subunit beta type-2Homo sapiens (human)
proteasome core complex, beta-subunit complexProteasome subunit beta type-2Homo sapiens (human)
cytosolProteasome subunit beta type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID781078Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis, and biological evaluation of bone-targeted proteasome inhibitors for multiple myeloma.
AID164126Inhibitory activity against 20S Proteasome1998Bioorganic & medicinal chemistry letters, Feb-17, Volume: 8, Issue:4
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.
AID264536Inhibition of trypsin-like proteasome activity of human 20S proteasome2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
AID781077Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Design, synthesis, and biological evaluation of bone-targeted proteasome inhibitors for multiple myeloma.
AID264539Inhibition of cathepsin S2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
AID264538Inhibition of cathepsin B2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
AID264537Inhibition of post glutamyl peptide hydrolase-like proteasome activity of human 20S proteasome2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
AID50483Inhibitory activity against Cathepsin B1998Bioorganic & medicinal chemistry letters, Feb-17, Volume: 8, Issue:4
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.
AID264535Inhibition of chymotrypsin-like proteasome activity of human 20S proteasome2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.86)18.2507
2000's26 (74.29)29.6817
2010's7 (20.00)24.3611
2020's1 (2.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.98

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.98 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index6.19 (4.65)
Search Engine Demand Index79.85 (26.88)
Search Engine Supply Index3.73 (0.95)

This Compound (34.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other35 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]