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  2. 誘導(dǎo)疾病模型產(chǎn)品 Metabolic Enzyme/Protease Apoptosis Protein Tyrosine Kinase/RTK
  3. 神經(jīng)系統(tǒng)疾病模型 Proteasome Apoptosis ROS Kinase
  4. 帕金森綜合癥模型
  5. Lactacystin

Lactacystin  (Synonyms: 蛋白酶體抑制劑)

目錄號(hào): HY-16594 純度: 98.2%
COA 產(chǎn)品使用指南

Lactacystin 是一種有效的、口服活性、不可逆的、細(xì)胞滲透性的，選擇性的 20S 蛋白酶體 (proteasome) 抑制劑 (IC50 = 4.8 μM)。Lactacystin 還能抑制溶酶體酶組織蛋白酶 A (cathepsin A)。Lactacystin 抑制細(xì)胞生長(zhǎng)，誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和周期阻滯，并具有抗病毒和抗氧化活性。Lactacystin 誘導(dǎo)神經(jīng)突生長(zhǎng)，誘發(fā)高血壓。Lactacystin 在癌癥、神經(jīng)系統(tǒng)疾病、高血壓和瘧疾等方面具有研究潛力。

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Lactacystin Chemical Structure

Lactacystin Chemical Structure

CAS No. : 133343-34-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
50 μg ￥1500
In-stock
100 μg ￥2400
In-stock
500 μg 現(xiàn)貨 詢價(jià)

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .

IC50 & Target

IC50: 4.8 μM (proteasome)[1]
體外研究
(In Vitro)

Lactacystin (高達(dá) 25.6 μM, 1 h) 對(duì) HeLa 和 SH-SY5Y 細(xì)胞無細(xì)胞毒性，可使 HeLa 細(xì)胞和 SH-SY5Y 細(xì)胞的 RVP 感染率分別降低 63.8% 和 74.5%[2]。
Lactacystin (2.5 μM) 聯(lián)合 Parthenolide (HY-N0141) (5 μM) 可協(xié)同增加耐藥 L1210 細(xì)胞的凋亡比例[3]。
Lactacystin (2.5, 5 和 10 μM, 24 h) 抑制 C6 細(xì)胞的增殖 (IC50 值為 10 μM)，增加凋亡[4]。
Lactacystin (10μM, 24 h) 增加 Hela 細(xì)胞內(nèi) Cisplatin (HY-17394) 誘導(dǎo)的內(nèi)質(zhì)網(wǎng)應(yīng)激相關(guān)的凋亡[5]。
Lactacystin (7.5 μM, 4-48 h) 可提高 HT-29 細(xì)胞的活性氧和谷胱甘肽水平[6]。
Lactacystin (1, 2.5, 5 μM, 24 h) 誘導(dǎo)新生大鼠皮質(zhì)星形膠質(zhì)細(xì)胞星性化[7]。
Lactacystin (10 μM, 8-24 h) 誘導(dǎo) PC12 細(xì)胞凋亡，G2/M 細(xì)胞周期阻滯[10]。

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

Cell Viability Assay[4]

Cell Line: C6 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Suppressed cell growth and viability to 28.9%, and increased the apoptotic in C6 cells.

Cell Viability Assay[10]

Cell Line: PC12
Concentration: 5, 10, 20 μM
Incubation Time: 24 h
Result: Declined cell viability in a concentration-dependent manner (79.47% at 5 mM, 49.31% at 10 μM and 31.20% at 20 μM.

Apoptosis Analysis[10]

Cell Line: PC12
Concentration: 10 μM
Incubation Time: 4, 8, 16, 24h
Result: Increased significantly apoptotic in a time-dependent manner from 8 to 24 h (14.10% at 8 h, 24.90% at 16 h and 39.41% at 24 h).

Cell Cycle Analysis[10]

Cell Line: PC12
Concentration: 10 μM
Incubation Time: 4, 8, 16, 24h
Result: Reduced in the number of cells in the G2-phase (from 17.45% to 30.94%, 31.80% and 32.18%, respectively.) of the cell cycle for 8, 16 and 24h.

RT-PCR[4][6]

Cell Line: C6 cells, HT-29 cells
Concentration: 0, 2.5, 5, and 10 μM (C6 cells）, 7.5 μM in HT-29 cells
Incubation Time: 24-48 h
Result: Increased the mRNA in the ratio of Bax to Bcl-2 in C6cells.
Increased the expression of GGT, GCLC, xCT and Nrf2 in HT-29 cells.

Western Blot Analysis[4][4]

Cell Line: C6 cells, HT-29 cells
Concentration: 0, 2.5, 5, and 10 μM (C6 cells）, 7.5 μM in HT-29 cells
Incubation Time: 24-48h
Result: Increased the expression in the ratio of Bax to Bcl-2 in C6cells.
Increased protein levels of GGT, GCLC, xCT in HT-29 cells.
體內(nèi)研究
(In Vivo)

Lactacystin (2 μg, ICV) 在注射后 5-7 天誘導(dǎo)年輕和成年小鼠帕金森病樣運(yùn)動(dòng)表型[8]。
Lactacystin (1.0 ug 或 5.0 μg/20 g，連續(xù)7天) 導(dǎo)致 C6 原位異種移植腫瘤模型腫瘤明顯縮小，并促進(jìn)組織凋亡[4]。
Lactacystin (5 mg/kg/每天，溶解在水中，給藥 6 周) 誘導(dǎo)成年雄性 Wistar 大鼠高血壓模型[9]。

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

Animal Model: Male C57Bl/6RccHsd mice with 8-9 weeks (young) and 12-14 months (adult) old[2]
Dosage: 2 μg
Administration: Microinjection
Result: Induced a Parkinson’s disease-like motor phenotype 5-7 days after injection in young and adult mice.
Animal Model: Male C57Bl/6RccHsd mice[8]
Dosage: 2 μg, 7days
Administration: Intracerebroventricular injection (ICV)
Result: Induced spontaneous contralateral rotating behavior.
Animal Model: C6 orthotopic xenograft tumor models[4]
Dosage: 1.0 ug or 5.0? μg/20g for 7days
Administration: Intravenous injection (i.p.)
Result: Reduced the tumor volume.
Showed polygonal condensed nuclei with brown Tunnel staining indicating apoptosis in tumor tissue.
Increased the mRNA and protein level in the ratio of Bax to Bcl-2 in tumor tissue.
分子量

376.43

Formula

C15H24N2O7S
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

蛋白酶體抑制劑
結(jié)構(gòu)分類
初始來源

Streptomyces?OM-6519
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)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 20 mg/mL (53.13 mM; 超聲加熱助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6565 mL 13.2827 mL 26.5654 mL
5 mM 0.5313 mL 2.6565 mL 5.3131 mL
查看完整儲(chǔ)備液配制表

* 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)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.2%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 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)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6565 mL 13.2827 mL 26.5654 mL 66.4134 mL
5 mM 0.5313 mL 2.6565 mL 5.3131 mL 13.2827 mL
10 mM 0.2657 mL 1.3283 mL 2.6565 mL 6.6413 mL
15 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4276 mL
20 mM 0.1328 mL 0.6641 mL 1.3283 mL 3.3207 mL
25 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6565 mL
30 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
40 mM 0.0664 mL 0.3321 mL 0.6641 mL 1.6603 mL
50 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
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產(chǎn)品名稱：
Lactacystin
目錄號(hào)：
HY-16594
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