MG-101
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MedKoo CAT#: 406548

CAS#: 110044-82-1

Description: MG-101, also known as Calpain Inhibitor I and ALLN, is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines. Activities of MG-101 includes: (1) reduce colon injury caused by dinitrobenzene sulphonic acid; (2) overcome acquired resistance to TRAIL; (3) protect against atractyloside-induced toxicity. (4). reduce colon injury caused by dinitrobenzene sulphonic acid.

Chemical Structure

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MG-101
CAS# 110044-82-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406548
Name: MG-101
CAS#: 110044-82-1
Chemical Formula: C20H37N3O4
Exact Mass: 383.28
Molecular Weight: 383.530
Elemental Analysis: C, 62.63; H, 9.72; N, 10.96; O, 16.69

Price and Availability

Size Price Availability Quantity
10mg USD 110 Ready to ship
25mg USD 210 Ready to ship
50mg USD 350 Ready to ship
100mg USD 600 Ready to ship
200mg USD 1050 Ready to ship
500mg USD 2150 Ready to ship
1g USD 3850 Ready to ship
2g USD 6250 Ready to ship
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Synonym: Calpain Inhibitor I; MG-101; MG 101; MG101; ALLN; AcLLnLCHO, Ac-Leu-Leu-Nle-Aldehyde.

IUPAC/Chemical Name: (S)-2-acetamido-4-methyl-N-((S)-4-methyl-1-oxo-1-(((R)-1-oxohexan-2-yl)amino)pentan-2-yl)pentanamide

InChi Key: FMYKJLXRRQTBOR-SQNIBIBYSA-N

InChi Code: InChI=1S/C20H37N3O4/c1-7-8-9-16(12-24)22-19(26)18(11-14(4)5)23-20(27)17(10-13(2)3)21-15(6)25/h12-14,16-18H,7-11H2,1-6H3,(H,21,25)(H,22,26)(H,23,27)/t16-,17+,18+/m1/s1

SMILES Code: CC(C)C[C@H](NC(C)=O)C(N[C@@H](CC(C)C)C(N[C@H](CCCC)C=O)=O)=O

Appearance: white 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, not in water

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:         

Biological target: MG-101 is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
In vitro activity: The cysteine protease inhibitor MG-101 counteracts the activity of lysosomal cathepsins L and B at a concentration of 20 nM or that of the non-lysosomal calpains I and II at 500 nM, respectively. Exposure of iBREC to either effective concentration of MG-101 together with aflibercept for 4 h resulted in a slight but significant increase of aflibercept isolated collectively with proteins from membranes and organelles (Fig. 5a). Because most of the intracellular protein destined to be degraded enters the ubiquitin-proteasome pathway, this study pre-treated iBREC with 20 nM of the inhibitor MG-132 of proteasomal proteases, before aflibercept was added to the cells for 4 h. Western blot analyses of proteins subsequently isolated from the membranes/organelles and the cytoskeleton revealed that more aflibercept accumulated during protease inhibition (Fig. 5b). As was to be expected, the amounts of endogenous proteins actin and claudin-5 were higher in samples isolated from cells treated with the inhibitors MG-101 or MG-132, confirming general inhibition of protein degradation pathways under these conditions (Fig. 5c, d). Higher concentrations of MG-101 or MG-132 could not be used because they resulted in barrier dysfunction and death of iBREC as recognized by cell index measurements. Reference: Graefes Arch Clin Exp Ophthalmol. 2019; 257(1): 83–94. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6323079/
In vivo activity: CI directly blocked the activation of calpain and prevented the rat heart against the proteolysis of α-fodrin, although CI may not protect the heart from other I/R injury. The present results showing decreased Ca2+ handling Vo2 in E-C coupling with unchanged oxygen costs of PVA and LV contractility probably reflect the decreased total amount of Ca2+ handled, which may be due to a suppression of the transsarcolemmal Ca2+ influx. The possibility that disruption of cytoskeletal proteins inactivate L-type Ca2+ channels has been reported. This study speculates that the linkage of the L-type Ca2+ channel to the membrane fodrin acts to tether the channel in place, which somehow modulates the basal activity of the channel, and a loss of the linkage may impair its regulation. Therefore, CI did not induce any conformational changes of the L-type Ca2+ channel at the cell membrane, resulting in protection of LV function associated with no impairment of the L-type Ca2+ channel function. Reference: Am J Physiol Heart Circ Physiol. 2005 Apr;288(4):H1690-8. https://pubmed.ncbi.nlm.nih.gov/15528229/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.6 97.93
DMF 20.0 52.15
Ethanol 48.0 121.15
Ethanol:PBS (pH 7.2) (1:1) 0.5 1.30

Preparing Stock Solutions

The following data is based on the product molecular weight 383.53 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. Deissler HL, Lang GK, Lang GE. Fate of the Fc fusion protein aflibercept in retinal endothelial cells: competition of recycling and degradation. Graefes Arch Clin Exp Ophthalmol. 2019 Jan;257(1):83-94. doi: 10.1007/s00417-018-4166-7. Epub 2018 Oct 26. PMID: 30367290; PMCID: PMC6323079. 2. Yoshikawa Y, Hagihara H, Ohga Y, Nakajima-Takenaka C, Murata KY, Taniguchi S, Takaki M. Calpain inhibitor-1 protects the rat heart from ischemia-reperfusion injury: analysis by mechanical work and energetics. Am J Physiol Heart Circ Physiol. 2005 Apr;288(4):H1690-8. doi: 10.1152/ajpheart.00666.2004. Epub 2004 Nov 4. PMID: 15528229. 4. Floyd ZE, Staszkiewicz J, Power RA, Kilroy G, Kirk-Ballard H, Barnes CW, Strickler KL, Rim JS, Harkins LL, Gao R, Kim J, Eilertsen KJ. Prolonged proteasome inhibition cyclically upregulates Oct3/4 and Nanog gene expression, but reduces induced pluripotent stem cell colony formation. Cell Reprogram. 2015 Apr;17(2):95-105. doi: 10.1089/cell.2014.0030. Erratum in: Cell Reprogram. 2015 Aug;17(4):323. Floyd, Elizabeth Z [corrected to Floyd, Z Elizabeth]. PMID: 25826722; PMCID: PMC4378358.
In vitro protocol: 1. Deissler HL, Lang GK, Lang GE. Fate of the Fc fusion protein aflibercept in retinal endothelial cells: competition of recycling and degradation. Graefes Arch Clin Exp Ophthalmol. 2019 Jan;257(1):83-94. doi: 10.1007/s00417-018-4166-7. Epub 2018 Oct 26. PMID: 30367290; PMCID: PMC6323079. 2. Floyd ZE, Staszkiewicz J, Power RA, Kilroy G, Kirk-Ballard H, Barnes CW, Strickler KL, Rim JS, Harkins LL, Gao R, Kim J, Eilertsen KJ. Prolonged proteasome inhibition cyclically upregulates Oct3/4 and Nanog gene expression, but reduces induced pluripotent stem cell colony formation. Cell Reprogram. 2015 Apr;17(2):95-105. doi: 10.1089/cell.2014.0030. Erratum in: Cell Reprogram. 2015 Aug;17(4):323. Floyd, Elizabeth Z [corrected to Floyd, Z Elizabeth]. PMID: 25826722; PMCID: PMC4378358.
In vivo protocol: 1. Yoshikawa Y, Hagihara H, Ohga Y, Nakajima-Takenaka C, Murata KY, Taniguchi S, Takaki M. Calpain inhibitor-1 protects the rat heart from ischemia-reperfusion injury: analysis by mechanical work and energetics. Am J Physiol Heart Circ Physiol. 2005 Apr;288(4):H1690-8. doi: 10.1152/ajpheart.00666.2004. Epub 2004 Nov 4. PMID: 15528229.

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1: Cheng XG, Su YP, Luo CJ, Liu XH. [Effect of calpain inhibitor I on ikappaBalpha expression and cytokine secretion in RAW264.7 cells attacked with LPS]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2006 Nov;22(6):720-2. Chinese. PubMed PMID: 17077009.

2: Zhu H, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther. 2004 May;9(5):666-73. PubMed PMID: 15120327.

3: Marzocco S, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S. Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44. PubMed PMID: 14676682.

4: Cuzzocrea S, Chatterjee PK, Mazzon E, Serraino I, Dugo L, Centorrino T, Barbera A, Ciccolo A, Fulia F, McDonald MC, Caputi AP, Thiemermann C. Effects of calpain inhibitor I on multiple organ failure induced by zymosan in the rat. Crit Care Med. 2002 Oct;30(10):2284-94. PubMed PMID: 12394957.

5: Ballinger A, Azooz O. Calpain inhibitor I and colonic inflammation induced by DNBS in the rat. Gut. 2002 Mar;50(3):440-1. PubMed PMID: 11839729; PubMed Central PMCID: PMC1773137.

6: Obatomi DK, Blackburn RO, Bach PH. Adenine nucleotide and calpain inhibitor I protect against atractyloside-induced toxicity in rat renal cortical slices in vitro. Arch Toxicol. 2001 Oct;75(8):487-96. PubMed PMID: 11757673.

7: Cuzzocrea S, McDonald MC, Mazzon E, Mota-Filipe H, Centorrino T, Terranova ML, Ciccolo A, Britti D, Caputi AP, Thiemermann C. Calpain inhibitor I reduces colon injury caused by dinitrobenzene sulphonic acid in the rat. Gut. 2001 Apr;48(4):478-88. PubMed PMID: 11247891; PubMed Central PMCID: PMC1728239.

8: McDonald MC, Mota-Filipe H, Paul A, Cuzzocrea S, Abdelrahman M, Harwood S, Plevin R, Chatterjee PK, Yaqoob MM, Thiemermann C. Calpain inhibitor I reduces the activation of nuclear factor-kappaB and organ injury/dysfunction in hemorrhagic shock. FASEB J. 2001 Jan;15(1):171-186. PubMed PMID: 11149905.

9: Cuzzocrea S, McDonald MC, Mazzon E, Siriwardena D, Serraino I, Dugo L, Britti D, Mazzullo G, Caputi AP, Thiemermann C. Calpain inhibitor I reduces the development of acute and chronic inflammation. Am J Pathol. 2000 Dec;157(6):2065-79. PubMed PMID: 11106579; PubMed Central PMCID: PMC1885785.

10: Sierra-Paredes G, Cornes JM, Sierra-Marcuño G. Calpain inhibitor I retards seizure offset in the hippocampus of freely moving rats. Neurosci Lett. 1999 Mar 26;263(2-3):165-8. PubMed PMID: 10213161.

11: Zhang L, Song L, Parker EM. Calpain inhibitor I increases beta-amyloid peptide production by inhibiting the degradation of the substrate of gamma-secretase. Evidence that substrate availability limits beta-amyloid peptide production. J Biol Chem. 1999 Mar 26;274(13):8966-72. PubMed PMID: 10085142.

12: Ruetten H, Thiemermann C. Effect of calpain inhibitor I, an inhibitor of the proteolysis of I kappa B, on the circulatory failure and multiple organ dysfunction caused by endotoxin in the rat. Br J Pharmacol. 1997 Jun;121(4):695-704. PubMed PMID: 9208136; PubMed Central PMCID: PMC1564738.

13: Milligan SA, Owens MW, Grisham MB. Inhibition of IkappaB-alpha and IkappaB-beta proteolysis by calpain inhibitor I blocks nitric oxide synthesis. Arch Biochem Biophys. 1996 Nov 15;335(2):388-95. PubMed PMID: 8914937.

14: Klafki HW, Paganetti PA, Sommer B, Staufenbiel M. Calpain inhibitor I decreases beta A4 secretion from human embryonal kidney cells expressing beta-amyloid precursor protein carrying the APP670/671 double mutation. Neurosci Lett. 1995 Dec 1;201(1):29-32. PubMed PMID: 8830305.

15: Fitzpatrick JS, Shahi K, Baudry M. Effect of seizure activity and calpain inhibitor I on LTP in juvenile hippocampal slices. Int J Dev Neurosci. 1992 Aug;10(4):313-9. PubMed PMID: 1384274.

16: Reichelt R, Möhler H, Hebebrand J. Calpain inhibitor I prevents rapid postmortem degradation of benzodiazepine binding proteins: fluorographic and immunological evidence. J Neurochem. 1990 Nov;55(5):1711-5. PubMed PMID: 2170581.