MG-132 (Z-Leu-Leu-Leu-al)

MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的，可逆的蛋白酶體 (proteasome) 抑制劑，IC50 為 100 nM。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛，是自噬 (autophagy) 激活劑。MG-132 還誘導(dǎo)凋亡 (apoptosis)。
貨號(hào)：HY-13259

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-13259

起訂量：1

規(guī)格:：10 mg

價(jià)格:：￥470

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產(chǎn)品詳情

MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的，可逆的蛋白酶體 (proteasome) 抑制劑，IC₅₀ 為 100 nM。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛，是自噬 (autophagy) 激活劑。MG-132 還誘導(dǎo)凋亡 (apoptosis)。

生物活性

MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC₅₀s 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]

體外研究
(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 IC₅₀ 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 IC₅₀ of 18.5 μM at 24 hours.

體內(nèi)研究
(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.

分子量

475.62

Formula

C₂₆H₄₁N₃O₅

CAS 號(hào)

133407-82-6

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline

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

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)

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

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil

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

參考文獻(xiàn)

[1]. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313.

[2]. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25.

[3]. 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.

[4]. Fiedler MA, et al. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132. Am J Respir Cell Mol Biol. 1998 Aug;19(2):259-68.

[5]. MacLaren AP, et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001 Mar;8(3):210-8.

[6]. 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.

[7]. Dang L, et al. Proteasome inhibitor MG132 inhibits the proliferation and promotes the cisplatin-inducedapoptosis of human esophageal squamous cell carcinoma cells. Int J Mol Med. 2014 May;33(5):1083-8.

[8]. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81.

[9]. Bonuccelli G, et al. Proteasome inhibitor (MG-132) treatment of mdx mice rescues the expression and membrane localization of dystrophin and dystrophin-associated proteins. Am J Pathol. 2003 Oct;163(4):1663-75.

MG-132 (Z-Leu-Leu-Leu-al)

MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的，可逆的蛋白酶體 (proteasome) 抑制劑，IC50 為 100 nM。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛，是自噬 (autophagy) 激活劑。MG-132 還誘導(dǎo)凋亡 (apoptosis)。
貨號(hào)：HY-13259

品牌：MCE

型號(hào)：HY-13259

起訂量：1

規(guī)格:：10 mg

價(jià)格:：￥470

15906629305

在線客服

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產(chǎn)品詳情

MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的，可逆的蛋白酶體 (proteasome) 抑制劑，IC₅₀ 為 100 nM。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛，是自噬 (autophagy) 激活劑。MG-132 還誘導(dǎo)凋亡 (apoptosis)。

生物活性

MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC₅₀s 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]

體外研究
(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 IC₅₀ 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 IC₅₀ of 18.5 μM at 24 hours.

體內(nèi)研究
(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.

分子量

475.62

Formula

C₂₆H₄₁N₃O₅

CAS 號(hào)

133407-82-6

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline

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

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)

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

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil

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