[CAS NO. 133407-82-6] MG-132

Name: MG-132
Brand: Arctom Scientific
SKU: AS466547

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PRODUCTS SPECIFICATIONS [133407-82-6]

Distributor

Catalog

AS466547

Brand

Arctom Scientific

CAS

133407-82-6

DESCRIPTION [133407-82-6]

Overview

MDL	MFCD00674886
Molecular Weight	475.62
Molecular Formula	C26H41N3O5
SMILES	O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C([H])=O)CC(C)C)=O)=O)CC(C)C

For research use only. We do not sell to patients.

545 Publications Citing Use of MCE

Summary

MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC ₅₀ s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis ^[1] ^[2] ^[3] .

IC50 & Target

IC50: 100 nM (Proteasome), 1.2 μM (Calpain) ^[1] ^[3]

In Vitro

MG-132 (Z-Leu-Leu-Leu-al) initiates neurite outgrowth in PC12 cells at a low concentration (30 nM) and is a very strong inhibitor of 20S proteasome ^[3] .
MG-132 (10 μM; 1 hour) reverses the effects of TNF- α on I κ B degradation and NF-κ B activation in A549 cells ^[4] .
MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition ^[5] .
MG-132 (10-40 μM; 24 hours) significantly reduces the viability of C6 glioma cells in both time- and concentration-dependent manners and shows the IC ₅₀ of 18.5 μM at 24 hours ^[6] .
MG-132 (18.5 μM; 24 hours) induces down-regulation of anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3 ^[6] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[3]

Cell Line:	C6 glioma cells
Concentration:	10, 20, 30, 40 μM
Incubation Time:	24 hours
Result:	Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC ₅₀ of 18.5 μM at 24 hours.

Western Blot Analysis ^[3]

Cell Line:	A549 cells
Concentration:	10 μM
Incubation Time:	1 hour
Result:	Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.

In Vivo

MG132 (10 mg/kg; i.p.; daily for 25 days starting 5 days after EC9706 cells injection) significantly inhibits tumor growth of the EC9706 xenograft without causing toxicity to mice ^[7] .
MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors ^[8] .
MG-132 (1-10 μg/kg/24 hours; subcutaneously implanted osmotic pumps; for 8 days) greatly increases the expression levels of β-dystroglycan, α-dystroglycan, α-sarcoglycan, and dystrophin in skeletal muscle lysates in mice (six-month-old male C57BL/10ScSn DMD mdx mice) ^[9] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5- to 6-weeks old female athymic nude mice (EC9706 xenograft)
Dosage:	10 mg/kg
Administration:	I.p.; daily for 25 days starting 5 days after EC9706 cells injection
Result:	Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.

Animal Model:	Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells) ^[8]
Dosage:	1 mg/kg
Administration:	Intravenous injection; twice a week for 4 weeks
Result:	The growth inhibition rates in HeLa tumors was 49% compared to the control.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 210.25 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1025 mL	10.5126 mL	21.0252 mL
5 mM	0.4205 mL	2.1025 mL	4.2050 mL
10 mM	0.2103 mL	1.0513 mL	2.1025 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.67 mg/mL (3.51 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 1.67 mg/mL (3.51 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.51 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

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)-

N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide

MG 132

Calpain inhibitor IV-2