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MG-132

カタログ番号 T2154   CAS 133407-82-6
別名: Z-LLL-al, Z-Leu-Leu-Leu-CHO

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

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MG-132 Chemical Structure
MG-132, CAS 133407-82-6
パッケージサイズ 在庫状況 単価(税別)
サンプルについてお問い合わせ
10 mg 在庫あり ¥ 9,500
25 mg 在庫あり ¥ 18,500
50 mg 在庫あり ¥ 34,000
100 mg 在庫あり ¥ 52,500
200 mg 在庫あり ¥ 91,000
500 mg 在庫あり ¥ 114,000
1 mL * 10 mM (in DMSO) 在庫あり ¥ 9,000
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生物学的特性に関する説明
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保存条件 & 溶解度情報
説明 MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.
ターゲット&IC50 20S proteasome:100 nM (cell free), Calpain:1.2 μM (cell free)
In vitro METHODS: Human cervical cancer cells HeLa were treated with MG-132 (0.5-30 μM) for 24 h, and cell growth inhibition was detected by MTT.
RESULTS: MG-132 dose-dependently inhibited HeLa cell growth with an IC50 of approximately 5 μM. [1]
METHODS: Human mesothelioma cells NCI-H2452 were treated with MG-132 (0.25-2 μM) for 36 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: MG-132 treatment induces cleavage of caspases 3 and 7, Bid, and PARP in NCI-H2452 cells. MG-132 induces a caspase-dependent apoptosis. [2]
METHODS: Human melanoma cells MeWo were treated with MG-132 (0.01-1 μM) for 24 h, and the cell cycle profiles were analyzed by Flow Cytometry.
RESULTS: MG-132 induces cell cycle arrest at G2 phase in MeWo cells. [3]
In vivo METHODS: To detect anti-tumor activity in vivo, MG-132 (1 mg/kg) was injected intravenously into C.B-17/lcr-scid/scidJcl mice harboring the human cervical cancer tumors HeLa, CaSki, or C33A twice a week for 4 weeks.
RESULTS: MG-132 significantly inhibited the growth of human cervical cancer tumors, indicating antitumor activity in vivo. [4]
METHODS: To investigate the effects of long-term treatment with MG-132 on cardiac hypertrophy and its associated molecular mechanisms, MG-132 (0.1 mg/kg) was injected intraperitoneally into rats with an abdominal aortic band (AAB) once daily for 8 weeks.
RESULTS: MG-132 treatment significantly attenuated left ventricular myocyte area, left ventricular weight/body weight, and lung weight/body weight ratios, decreased left ventricular diastolic diameter and wall thickness, and increased the shortening fraction in AAB rats. MG-132 treatment significantly reversed the elevated levels of ERK1/2 and JNK1 phosphorylation in AAB rats. [5]
キナーゼ試験 Inhibitory activities of ZLLa1 and ZLLLal against m-calpain and 20S proteasome were measured by previously described methods.For the m-calpain inhibitory assay,the 0.5 ml reaction mixture contained 0.24% alkali-denatured casein,28 mM 2-mercaptoethanol,0.94 unit of m-calpain,ZLLal or ZLLLal,6 mM CaCl2,and 0.1M Tris-HC1 (pH 7.5).The reaction was started by the addition of m-calpain solution and stopped by the addition of 0.5 ml of 10% trichloroacetic acid after incubation at 30℃ for 15 min.After centrifugation at 1,300×g for 10 min,the absorbance of the supernatant at 280 nm was measured.The reaction mixture for the 20S proteasome inhibitory assay contained 0.1 M Tris-acetate,pH 7.0,20S proteasome,ZLLa1 or ZLLLal,and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 ml.After incubation at 37℃ for 15 min,the reaction was stopped by the addition of 0.1 ml of 10% SDS and 0.9 ml of 0.1 M Tris-acetate,pH 9.0.The fluorescence of the reaction products was measured.To determine the IC50s against m-calpain and 20S proteasome,various concentrations of the synthetic peptide aldehydes were included in the assay mixture [1].
細胞研究 The effect of MG132 on HeLa cell growth was determined by trypan blue exclusion cell counting or measuring MTT dye absorbance of living cells as previously described. In brief, cells (5x10^5 cells per well) were seeded in 24-well plates for cell counting, and cells (5x10^4 cells per well) were seeded in 96-well microtiter plates for the MTT assay. After exposure to indicated amounts of MG132 for 24 h, cells in 24-well plates or 96-well plates were collected with trypsin digestion for trypan blue exclusion cell counting or were used for the MTT assay. Twenty microliters of MTT solution (2 mg/ml in PBS) was added to each well of 96-well plates. The plates were again incubated for 4 h at 37?C. MTT solution in the medium was aspirated off and 200 μl of DMSO was added to each well to solubilize the formazan crystals formed in viable cells. Optical density was measured at 570 nm using a microplate reader. Each plate contained multiple wells at a given experimental condition and multiple control wells. This procedure was replicated for 2-4 plates per condition [3].
動物実験 Male Sprague–Dawley rats (8 weeks old, 180 – 230 g) were used to establish a pressure-overload model as described previously. All animals were separated into four groups (10 rats per group): (i) vehicle-treated sham group; (ii) MG132-treated sham group; (iii) vehicle-treated abdominal aortic banding (AAB) group; and (iv) MG132-treated AAB group. Under intraperitoneal pentobarbital (50 mg/kg) anesthesia, AAB was created using a 5-0 suture tied twice around the abdominal aorta in which. a 21-gauge needle was inserted. The needle was then retracted yielding a 70 – 80% constriction with an outer aortic diameter of 0.8 mm. In the sham surgery rats, the same surgery was performed as described above except the aorta was constricted. At Day 3 after the surgery, MG132-treated rats were intraperitoneally injected with 0.1 mg/kg/day of MG132 for 8 weeks. All control animals were injected with a corresponding volume of vehicle only (0.1% DMSO) [4]. Sixteen-week-old male CD1 mice were used for all our experiments. Thirty minutes before the immobilization procedure, 0.1 mg/kg of buprenorphine was administrated IP. The mice were then anesthetized using isoflurane. The right hindlimb was immobilized as previously described. Briefly, the hindlimb was immobilized 7 days by stapling the foot exploiting normal dorso-tibial flexion using an Autosuture Royal 35W skin stapler. One tine was inserted close to the toe at the plantar portion of the foot while the other was inserted in the distal portion of the gastrocnemius. The other hindlimb was used as a control. During the immobilization period, the mice were injected subcutaneously with MG132 (7.5 mg/kg/dose) or vehicle (DMSO) twice daily. DMSO containing or not MG132 was diluted in sterile pure corn oil (1:100, injected volume 150 μL). After 7 days, the tibialis anterior (TA) muscles of immobilized and non-i
別名 Z-LLL-al, Z-Leu-Leu-Leu-CHO
分子量 475.62
分子式 C26H41N3O5
CAS No. 133407-82-6

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

H2O: Insoluble

Ethanol: 47.5 mg/mL (100 mM)

DMSO: 45 mg/mL (94.61 mM)

参考文献

1. Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 2009 Jul;22(1):215-21. 2. Yuan BZ, et al. Proteasome Inhibitor MG132 Induces Apoptosis and Inhibits Invasion of Human Malignant Pleural Mesothelioma Cells. Transl Oncol. 2008 Sep;1(3):129-40. 3. Braun HA, et al. Tripeptide mimetics inhibit the 20 S proteasome by covalent bonding to the active threonines. J Biol Chem. 2005 Aug 5;280(31):28394-401. 4. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating the proteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81. 5. Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure-overload-induced cardiac hypertrophy in rats by modulation of mitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai). 2010 Apr;42(4):253-8. 6. Caron AZ, et al. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185. 7. Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6. 8. Guzmán-Téllez P, Martínez-Valencia D, Silva-Olivares A, et al. Naegleria fowleri and Naegleria gruberi 20S proteasome: identification and characterization[J]. European Journal of Cell Biology. 2020: 151085

引用文献

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投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか?
[分子量(MW)]の欄に[197.13]と入力してください
[濃度]ボックスに10と入力し、正しい単位(millimolar)を選択します
[容量]ボックスに10と入力し、正しい単位(milliliter)を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2&V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか?
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度(開始)ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度(終了)ボックスに50を入力し正しい単位(millimolar)を選択してください
体積(終了)ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積(開始)ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント:化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量(分子量)を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量(分子量)とは、物質の1分子の質量であり、統一された原子質量単位(u)で表されます。(1uは炭素12の1原子の質量の1/12に等しい)
モル質量(molar weight)とは、ある物質の1モルの質量のことで、単位はg/molです。

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Keywords

MG-132 133407-82-6 Apoptosis Autophagy Proteases/Proteasome Ubiquitination Proteasome Inhibitor MG 132 complex peptide calpain MG132 Z-LLL-al proteolytic aldehyde inhibit Z-Leu-Leu-Leu-CHO 26S inhibitor