MG-101 (ALLN)

Catalog No.S7386 Synonyms: Calpain inhibitor-1, Ac-LLnL-CHO

For research use only.

MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

MG-101 (ALLN) Chemical Structure

CAS No. 110044-82-1

Selleck's MG-101 (ALLN) has been cited by 15 publications

Purity & Quality Control

Choose Selective Cysteine Protease Inhibitors

Biological Activity

Description MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
Targets
Cysteine protease [1]
In vitro

MG-101 (ALLN) effectively inhibits cysteine proteinases with ID50 of 7 nM and 13 nM for cathepsins L and B, respectively. MG-101 (ALLN) shows very weak inhibitory activities towards cathepsin D (aspartic protease) and subtilisin (serine protease). MG-101 thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. [1] MG-101, as an inhibitor of Ca(2+)-dependent cysteine proteases, inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. [2] In HCT116 cells, MG-101 decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L1210 M4D1e2Z2dmO2aX;uJIF{e2G7 M{PvcWlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDv[kB1cGViY3;tdI92dmRid3HzJIRmfGW{bXnu[YQh[WejaX7zeEBNOTJzMDDj[YxteyxiSVO1NF0{|ryPLh?= M4Ltd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NkO0NFI5Lz5zNU[zOFAzQDxxYU6=
melanoma B16 MkHOSpVv[3Srb36gZZN{[Xl? NFyxS2NKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gc4YhfGinIHPvcZBwfW6mIIfhd{Bl\XSncn3pcoVlKGGpYXnud5QhdWWuYX7vcYEhSjF4IHPlcIx{NCCLQ{WwQVE1NjYQvF2u MnT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV4M{SwNlgoRjF3NkO0NFI5RC:jPh?=
HeLa M{jJW2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGXaXpA1QCCqcoO= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFNiYYPzZZktKEOFNUC9NlUvOc7:TT6= M1\tXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{W3OlMzLz5{M{O1O|Y{OjxxYU6=
HEK293 M122OWZ2dmO2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKHC{b4TlZZNwdWViZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gR5lkdGmwREGtR2RMPCCrboTldoFkfGmxbjDjc41xdGW6ZYOgZpkhTVmIUDDhcoQwd3JiWV\QJHZmdnW|IH\yZYdu\W62IHLhd4VlKHKncH;yeIVzKGenbnWgZZN{[Xl? NFzZUoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNk[4NFE2QSd-MU[2PFAyPTl:L3G+
HEK293 NIXPUZZHfW6ldHnvckBie3OjeR?= MnnNTY5pcWKrdHnvckBw\iCycn;0[YF{d22nIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJHBqdjFvSoXuJIlvfGW{YXP0bY9vKGOxbYDs[ZhmeyCkeTDFXWZRKGGwZD;vdkB[TlBiVnXueZMh\nKjZ33lcpQh[mG|ZXSgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ6MEG1PUc,OTZ4OECxOVk9N2F-
HEK293 MWHGeY5kfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKHC{b4TlZZNwdWViZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gdFU{NXB3MzDpcpRmemGldHnvckBkd22ybHX4[ZMh[nliRWnGVEBidmRxb4KgXWZRKF[nboXzJIZz[WevZX70JIJie2WmIILldI9zfGW{IHflcoUh[XO|YYm= M3XPUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NkiwNVU6Lz5zNk[4NFE2QTxxYU6=
HEK293 NHHQVWlHfW6ldHnvckBie3OjeR?= M1;LemVn\mWldDDvckBkd2[rbHnuNUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGWoZnXjeEBwdiClb3\pcIlvOTtiTHntb|IhcW62ZYLhZ5Rqd25iY3;tdIxmgGW|IHL5JGV[TlBiYX7kM49zKFmIUDDW[Y52eyCocnHncYVvfCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 NIrtUVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNk[4NFE2QSd-MU[2PFAyPTl:L3G+
HEK293 MX\GeY5kfGmxbjDhd5NigQ>? M1PvWWlvcGmkaYTpc44hd2ZicILveIVie2:vZTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIVn\mWldDDvckBGPjqHNlHQJIlvfGW{YXP0bY9vKGOxbYDs[ZhmeyCkeTDFXWZRKGGwZD;vdkB[TlBiVnXueZMh\nKjZ33lcpQh[mG|ZXSgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NGGwWY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNk[4NFE2QSd-MU[2PFAyPTl:L3G+
HEK293 MV;GeY5kfGmxbjDhd5NigQ>? NH3GW4ZKdmirYnn0bY9vKG:oIIDyc5Rm[XOxbXWg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{Bm\m[nY4Sgc44heDV|LVPob|EhcW62ZYLhZ5Rqd25iY3;tdIxmgGW|IHL5JGV[TlBiYX7kM49zKFmIUDDW[Y52eyCocnHncYVvfCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 NWnhXldGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[2PFAyPTlpPkG2OlgxOTV7PD;hQi=>
Assay
Methods Test Index PMID
Western blot Cyclin D3 / Cyclin D1 / CDK4 / CDK6 ; p21(WAF1/CIP1) 28130444
In vivo In mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation. [3]

Protocol (from reference)

Cell Research:[3]
  • Cell lines: HCT116, HCT116/p53−/−, and HCT116/Bax−/− cells
  • Concentrations: ~26 μM
  • Incubation Time: 24 hours
  • Method: Cells viability is assayed using Cell Counting Kit-8 following manufacturer’s protocol. All HCT116 cell typesare seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of ALLN for 24 h. Medium is then replaced by 100 μl fresh McCoy’s 5A complete medium with 10% CCK-8 reagent and incubated for 1 h. Absorbance is measured at 450 nm using a microplate reader. Results are shown as death percentages.
Animal Research: [3]
  • Animal Models: Female athymic nude mice bearing HCT116 xenografts
  • Dosages: 10 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 383.53
Formula

C20H37N3O4

CAS No. 110044-82-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04987242 Recruiting Drug: ALLN-346|Drug: Placebo Hyperuricemia|Gout Allena Pharmaceuticals July 16 2021 Phase 2
NCT04829435 Completed Drug: ALLN-346|Drug: Placebo Hyperuricemia|Gout Allena Pharmaceuticals April 21 2021 Phase 1
NCT04236219 Completed Drug: ALLN-346|Drug: Placebo Hyperuricemia Allena Pharmaceuticals September 2 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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