Drug Details

General Information of the Drug (ID: DR3952)
Name
MG132
Synonyms
MG-132; 133407-82-6; Z-Leu-leu-leu-al; MG132; MG 132; Zlllal; Z-LLL-CHO; Zlll-cho; Z-Leu-leu-leucinal; Z-Leu-Leu-Leu-H; Carbobenzoxy-leucyl-leucyl-leucinal; UNII-RF1P63GW3K; Benzyloxycarbonyl-leu-leu-leu-aldehyde; Benzyloxycarbonyl-leucyl-leucyl-leucinal; Carbobenzoxyl-leucinyl-leucinyl-leucinal-H; Cbz-Leu-Leu-Leu-H; C26H41N3O5; Benzyloxycarbonylleucyl-leucyl-leucine aldehyde; Z-Leu-Leu-Leu-aldehyde; RF1P63GW3K; Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal; CHEMBL64925; benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate; Cbz-L-Leu-L-Leu-L-Leu-CHO; CHEBI:75142; MFCD00674886; Benzyl ((S)-4-methyl-1-(((S)-4-methyl-1-(((S)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)carbamate; Lll cpd; (S)-N-((Phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-3-methylbutyl)-L-leucinamide; N-[(Benzyloxy)carbonyl]-L-Leucyl-N-[(2s)-4-Methyl-1-Oxopentan-2-Yl]-L-Leucinamide; BRD0970; BRD-0970; Z-LLL; N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide; (R)-MG132; (S)-MG132; N-[(benzyloxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide; Z-LLL-aldehyde; 1211877-36-9; Benzyl N-[(1S)-3-methyl-1-[[(1S)-3-methyl-1-[[(2S)-4-methyl-1-oxo-pentan-2-yl]carbamoyl]butyl]carbamoyl]butyl]carbamate; Z-LLLal; Cbz-Leu-Leu-Leu-al; Cbz-Leu-Leu-Leucinal; Z-LLL-H; Z-L-leu-L-leu-L-leu-H; BSPBio_001310; carbobenzoxy-Leu-Leu-leucinal; KBioGR_000030; KBioSS_000030; cc-245; MLS006011220; Cbz-L-Leu-L-Leu-L-Leu-H; SCHEMBL160925; GTPL8616; DTXSID3042639; BCBcMAP01_000028; KBio2_000030; KBio2_002598; KBio2_005166; KBio3_000059; KBio3_000060; AOB4946; QCR-183; benzyloxycarbonyl-Leu-Leu-leucinal; Bio2_000030; Bio2_000510; HMS1361B12; HMS1791B12; HMS1989B12; HMS3402B12; AMY40914; EX-A1500; ABP000958; BDBM50069985; NSC782153; PI-102; s2619; ZINC13476439; AKOS027420457; MG132/MG-132/; ACN-047884; CCG-207860; CCG-208036; CS-0471; NSC-782153; SB19111; compound 5b [PMID: 16686537]; IDI1_033780; NCGC00161679-01; NCGC00161679-02; NCGC00161679-03; NCGC00161679-04; Z-Leu-Leu-Leu-al, >=90% (HPLC); AS-55854; HY-13259; SMR002530629; AB0033810; SW219780-1; UNM000011053701; X7579; W-5117; InSolution MG-132 - CAS 133407-82-6; n-benzyloxycarbonyl-l-leucyl-l-leucyl-l-leucinal; Q3272916; SR-01000864598-1; BRD-K60230970-001-04-3; BRD-K60230970-001-05-0; BRD-K60230970-001-06-8; BRD-K60230970-001-07-6; BRD-K60230970-001-08-4; BRD-K60230970-001-10-0; MG-132 - CAS 133407-82-6; MG-132, >/=95% by HPLC - CAS 133407-82-6; L-Leucinamide, N-((phenylmethoxy)carbonyl)-L-leucyl-N-((1S)-1-formyl-3-methylbutyl)-; L-Leucinamide, N-((phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-3-methylbutyl)-, (S)-; L-Leucinamide, N-[(phenylmethoxy)carbonyl]-L-leucyl-N1-[(1S)-1-formyl-3-methylbutyl]-; N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-(1-formyl-3-methylbutyl)-(S)-L-leucinamide; (S)-4-methyl-2-(3-phenyl-propionylamino)-pentanoic acid [(S)-1-((S)-1-formyl-3-methyl-butylcarbamoyl)-3-methyl-butyl]-amide; {(S)-1-[(S)-1-((S)-1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester; {1-[(S)-(S)-1-((S)-1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester; {1-[1-(1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester; benzyl N-[(1S)-1-[[(1S)-1-[[(1S)-1-formyl-3-methyl-butyl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-butyl]carbamate; benzyl(S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate; phenylmethyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
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Molecular Type
Small molecule
Disease Lung cancer [ICD-11: 2C25] Investigative [1]
Structure
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2D MOL

3D MOL

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Formula
C26H41N3O5
PubChem CID
462382
Canonical SMILES
CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
InChI
1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1
InChIKey
TZYWCYJVHRLUCT-VABKMULXSA-N
CAS Number
CAS 133407-82-6
ChEBI ID
CHEBI:75142
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Arsenic trioxide      Realgar and orpiment     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Up-regulation Expression BNIP3  Molecule Info 
Pathway MAP
Up-regulation Expression MAP1LC3A  Molecule Info 
Pathway MAP
                    In-vitro Model U-937 CVCL_0007 Adult acute monocytic leukemia Homo sapiens
Raji CVCL_0511 EBV-related Burkitt lymphoma Homo sapiens
                    Experimental
                    Result(s)		 Synergism between ATO and MG132 was attained in Raji cells by disruption of the perinuclear mitochondrial cluster, blockage of selective autophagy of mitochondria (mitophagy) by VCR, increased mitochondrial mass, and upregulation of BNIP3 by VPA.
          Gambogic acid      Garcinia morella     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [3]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Up-regulation Cleavage PARP1  Molecule Info 
Pathway MAP
                    In-vitro Model K-562 CVCL_0004 Chronic myelogenous leukemia Homo sapiens
H22 CVCL_H613 Hepatocellular carcinoma of the mouse Mus musculus
                    In-vivo Model Murine hepatoma H22 cells (10 * 106) suspended in 0.2 ml of serum-free RPMI 1640 were inoculated s.c. in the left armpit of each mouse.
                    Experimental
                    Result(s)		 The combination of natural product gambogic acid and the proteasome inhibitor MG132 or MG262 results in a synergistic inhibitory effect on growth of malignant cells and tumors in allograft animal models and there was no apparent systemic toxicity observed in the animals treated with the combination.
Target and Pathway
Target(s) Glucose-dependent insulinotropic receptor (GPR119)  Molecule Info  [4]
KEGG Pathway cAMP signaling pathway Click to Show/Hide
2 Insulin secretion
WikiPathways Incretin Synthesis, Secretion, and Inactivation Click to Show/Hide
References
Reference 1 MG132 enhances the radiosensitivity of lung cancer cells in vitro and in vivo. Oncol Rep. 2015 Oct;34(4):2083-9.
Reference 2 Synergism of arsenic trioxide and MG132 in Raji cells attained by targeting BNIP3, autophagy, and mitochondria with low doses of valproic acid and vincristine. Eur J Cancer. 2014 Dec;50(18):3243-61.
Reference 3 Gambogic acid enhances proteasome inhibitor-induced anticancer activity. Cancer Lett. 2011 Feb 28;301(2):221-8.
Reference 4 Synergistic Effects of a GPR119 Agonist with Metformin on Weight Loss in Diet-Induced Obese Mice. J Pharmacol Exp Ther. 2015 Jun;353(3):496-504.
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