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MedKoo Cat#: 562247 | Name: MG115
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MG115 is an inhibitor of NFκB in the cytoplasm by acting on IKK or the proteasome.

Chemical Structure

MG115
MG115
CAS#133407-86-0

Theoretical Analysis

MedKoo Cat#: 562247

Name: MG115

CAS#: 133407-86-0

Chemical Formula: C25H39N3O5

Exact Mass: 461.2890

Molecular Weight: 461.60

Elemental Analysis: C, 65.05; H, 8.52; N, 9.10; O, 17.33

Price and Availability

Size Price Availability Quantity
50mg USD 950.00 2 Weeks
100mg USD 1,650.00 2 Weeks
200mg USD 2,950.00 2 Weeks
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Related CAS #
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Synonym
MG115; MG-115; MG 115; Z-LL-Nva-CHO; ASD 4955; ASD-4955; ASD4955; Z-Leu-Leu-Norvalinal; Z-LLnV
IUPAC/Chemical Name
Benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
InChi Key
QEJRGURBLQWEOU-FKBYEOEOSA-N
InChi Code
InChI=1S/C25H39N3O5/c1-6-10-20(15-29)26-23(30)21(13-17(2)3)27-24(31)22(14-18(4)5)28-25(32)33-16-19-11-8-7-9-12-19/h7-9,11-12,15,17-18,20-22H,6,10,13-14,16H2,1-5H3,(H,26,30)(H,27,31)(H,28,32)/t20-,21-,22-/m0/s1
SMILES Code
O=C(OCC1=CC=CC=C1)N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC)C=O)=O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome.
In vitro activity:
Programmed cell death (PCD) is a crucial process in plant development. In this paper, proteolytically related aspects of kinetin-induced PCD in cortex cells of Vicia faba ssp. minor seedlings were examined using morphological, fluorometric, spectrophotometric, and fluorescence microscopic analyses. N-ethylmaleimide (NEM), phenylmethylsulfonyl fluoride (PMSF), and Z-Leu-Leu-Nva-H (MG115), the respective cysteine, serine, and proteasome inhibitors, suppressed kinetin-induced PCD. Addition of proteasome inhibitor MG-115 reduced the number of dying cells, suggesting that proteasomes might play an important role during kinetin-induced PCD. Reference: Protoplasma. 2017 Nov;254(6):2273-2285. https://pubmed.ncbi.nlm.nih.gov/28501974/
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 25.0 54.16
Ethanol 30.0 64.99
Ethanol:PBS (pH 7.2) (1:3) 0.3 0.54
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 461.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kaźmierczak A, Doniak M, Kunikowska A. Proteolytic activities in cortex of apical parts of Vicia faba ssp. minor seedling roots during kinetin-induced programmed cell death. Protoplasma. 2017 Nov;254(6):2273-2285. doi: 10.1007/s00709-017-1119-7. Epub 2017 May 13. PMID: 28501974. 2. Kim J, Chen CP, Rice KG. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90. doi: 10.1038/sj.gt.3302575. PMID: 16034460.
In vitro protocol:
1. Kaźmierczak A, Doniak M, Kunikowska A. Proteolytic activities in cortex of apical parts of Vicia faba ssp. minor seedling roots during kinetin-induced programmed cell death. Protoplasma. 2017 Nov;254(6):2273-2285. doi: 10.1007/s00709-017-1119-7. Epub 2017 May 13. PMID: 28501974. 2. Kim J, Chen CP, Rice KG. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90. doi: 10.1038/sj.gt.3302575. PMID: 16034460.
In vivo protocol:
TBD
1: Kaźmierczak A, Doniak M, Kunikowska A. Proteolytic activities in cortex of apical parts of Vicia faba ssp. minor seedling roots during kinetin-induced programmed cell death. Protoplasma. 2017 Nov;254(6):2273-2285. doi: 10.1007/s00709-017-1119-7. Epub 2017 May 13. PubMed PMID: 28501974. 2: Kim A, Nam YJ, Lee MS, Shin YK, Sohn DS, Lee CS. Apigenin Reduces Proteasome Inhibition-Induced Neuronal Apoptosis by Suppressing the Cell Death Process. Neurochem Res. 2016 Nov;41(11):2969-2980. Epub 2016 Jul 29. PubMed PMID: 27473386. 3: Nam YJ, Kim A, Lee MS, Shin YK, Sohn DS, Lee CS. Lamotrigine Attenuates Proteasome Inhibition-Induced Apoptosis by Suppressing the Activation of the Mitochondrial Pathway and the Caspase-8- and Bid-Dependent Pathways. Neurochem Res. 2016 Oct;41(10):2503-2516. Epub 2016 May 26. PubMed PMID: 27230883. 4: Nam YJ, Lee DH, Lee MS, Lee CS. K(ATP) channel block prevents proteasome inhibitor-induced apoptosis in differentiated PC12 cells. Eur J Pharmacol. 2015 Oct 5;764:582-91. doi: 10.1016/j.ejphar.2015.06.049. Epub 2015 Jul 2. PubMed PMID: 26142827. 5: Katayama K, Kapoor K, Ohnuma S, Patel A, Swaim W, Ambudkar IS, Ambudkar SV. Revealing the fate of cell surface human P-glycoprotein (ABCB1): The lysosomal degradation pathway. Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2361-70. doi: 10.1016/j.bbamcr.2015.06.001. Epub 2015 Jun 6. PubMed PMID: 26057472; PubMed Central PMCID: PMC4558211. 6: Bellizzi A, White MK, Wollebo HS. Degradation of polyomavirus JC T-antigen by stress involves the LIP isoform of C/EBP. Cell Cycle. 2015;14(13):2075-9. doi: 10.1080/15384101.2015.1042631. Epub 2015 May 27. PubMed PMID: 26017382; PubMed Central PMCID: PMC4615132. 7: Nam YJ, Lee DH, Shin YK, Sohn DS, Lee CS. Flavanonol taxifolin attenuates proteasome inhibition-induced apoptosis in differentiated PC12 cells by suppressing cell death process. Neurochem Res. 2015 Mar;40(3):480-91. doi: 10.1007/s11064-014-1493-x. Epub 2014 Dec 5. PubMed PMID: 25476842. 8: Brojatsch J, Lima H, Kar AK, Jacobson LS, Muehlbauer SM, Chandran K, Diaz-Griffero F. A proteolytic cascade controls lysosome rupture and necrotic cell death mediated by lysosome-destabilizing adjuvants. PLoS One. 2014 Jun 3;9(6):e95032. doi: 10.1371/journal.pone.0095032. eCollection 2014. PubMed PMID: 24893007; PubMed Central PMCID: PMC4043491. 9: Nam YJ, Lee DH, Kim YJ, Shin YK, Sohn DS, Lee MS, Lee CS. 3,4,5-tricaffeoylquinic acid attenuates proteasome inhibition-mediated programmed cell death in differentiated PC12 cells. Neurochem Res. 2014 Aug;39(8):1416-25. doi: 10.1007/s11064-014-1327-x. Epub 2014 May 14. PubMed PMID: 24825618. 10: Jung EB, Lee CS. Baicalein attenuates proteasome inhibition-induced apoptosis by suppressing the activation of the mitochondrial pathway and the caspase-8- and Bid-dependent pathways. Eur J Pharmacol. 2014 May 5;730:116-24. doi: 10.1016/j.ejphar.2014.02.039. Epub 2014 Mar 12. PubMed PMID: 24631255. 11: Agholme L, Nath S, Domert J, Marcusson J, Kågedal K, Hallbeck M. Proteasome inhibition induces stress kinase dependent transport deficits--implications for Alzheimer's disease. Mol Cell Neurosci. 2014 Jan;58:29-39. doi: 10.1016/j.mcn.2013.11.001. Epub 2013 Nov 21. PubMed PMID: 24270002. 12: Huang W, Miao M, Kud J, Niu X, Ouyang B, Zhang J, Ye Z, Kuhl JC, Liu Y, Xiao F. SlNAC1, a stress-related transcription factor, is fine-tuned on both the transcriptional and the post-translational level. New Phytol. 2013 Mar;197(4):1214-24. doi: 10.1111/nph.12096. Epub 2012 Dec 21. Erratum in: New Phytol. 2013 Oct;200(1):284. PubMed PMID: 23278405. 13: Agholme L, Hallbeck M, Benedikz E, Marcusson J, Kågedal K. Amyloid-β secretion, generation, and lysosomal sequestration in response to proteasome inhibition: involvement of autophagy. J Alzheimers Dis. 2012;31(2):343-58. doi: 10.3233/JAD-2012-120001. PubMed PMID: 22555375. 14: Sakurai T, Kudo M, Itoh K, Ryu U, Higashitsuji H, Fujita J. Adriamycin enhances proteasome-mediated generation of the proapoptotic processed form of MAGE-A4 in hepatoma cells. Oncology. 2011;81 Suppl 1:30-5. doi: 10.1159/000334307. Epub 2011 Dec 22. PubMed PMID: 22212933. 15: Pérez-Pertejo Y, Alvarez-Velilla R, Estrada CG, Balaña-Fouce R, Reguera RM. Leishmania donovani: proteasome-mediated down-regulation of methionine adenosyltransferase. Parasitology. 2011 Aug;138(9):1082-92. doi: 10.1017/S0031182011000862. PubMed PMID: 21813028. 16: Xing W, Pourteymoor S, Mohan S. Ascorbic acid regulates osterix expression in osteoblasts by activation of prolyl hydroxylase and ubiquitination-mediated proteosomal degradation pathway. Physiol Genomics. 2011 Jun 28;43(12):749-57. doi: 10.1152/physiolgenomics.00229.2010. Epub 2011 Apr 5. PubMed PMID: 21467157; PubMed Central PMCID: PMC4459927. 17: Liu TY, Wu SJ, Huang MH, Lo FY, Tsai MH, Tsai CH, Hsu SM, Lin CW. EBV-positive Hodgkin lymphoma is associated with suppression of p21cip1/waf1 and a worse prognosis. Mol Cancer. 2010 Feb 9;9:32. doi: 10.1186/1476-4598-9-32. PubMed PMID: 20144199; PubMed Central PMCID: PMC2834611. 18: Ohtani M, Numazaki M, Yajima Y, Fujita-Yamaguchi Y. Mechanisms of antibody-mediated insulin-like growth factor I receptor (IGF-IR) down-regulation in MCF-7 breast cancer cells. Biosci Trends. 2009 Aug;3(4):131-8. PubMed PMID: 20103837. 19: Gartel AL. A new target for proteasome inhibitors: FoxM1. Expert Opin Investig Drugs. 2010 Feb;19(2):235-42. doi: 10.1517/13543780903563364. Review. PubMed PMID: 20074015; PubMed Central PMCID: PMC3532816. 20: Torrice A, Cardinale V, Gatto M, Semeraro R, Napoli C, Onori P, Alpini G, Gaudio E, Alvaro D. Polycystins play a key role in the modulation of cholangiocyte proliferation. Dig Liver Dis. 2010 May;42(5):377-85. doi: 10.1016/j.dld.2009.09.008. Epub 2009 Nov 7. PubMed PMID: 19897428.