1. 诱导疾病模型产品 Metabolic Enzyme/Protease Apoptosis Protein Tyrosine Kinase/RTK
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  4. Lactacystin

Lactacystin  (Synonyms: 蛋白酶体抑制剂)

目录号: HY-16594
COA 产品使用指南

Lactacystin 是一种有效的、口服活性、不可逆的、细胞渗透性的,选择性的 20S 蛋白酶体 (proteasome) 抑制剂 (IC50 = 4.8 μM)。Lactacystin 还能抑制溶酶体酶组织蛋白酶 A (cathepsin A)。Lactacystin 抑制细胞生长,诱导细胞凋亡 (apoptosis) 和周期阻滞,并具有抗病毒和抗氧化活性。Lactacystin 诱导神经突生长,诱发高血压。Lactacystin 在癌症、神经系统疾病、高血压和疟疾等方面具有研究潜力。

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Lactacystin Chemical Structure

Lactacystin Chemical Structure

CAS No. : 133343-34-7

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]

体外研究
(In Vitro)

Lactacystin (高达 25.6 µM, 1 h) 对 HeLa 和 SH-SY5Y 细胞无细胞毒性,可使 HeLa 细胞和 SH-SY5Y 细胞的 RVP 感染率分别降低 63.8% 和 74.5%[2]
Lactacystin (2.5 μM) 联合 Parthenolide (HY-N0141) (5 μM) 可协同增加耐药 L1210 细胞的凋亡比例[3]
Lactacystin (2.5, 5 和 10 µM, 24 h) 抑制 C6 细胞的增殖 (IC50 值为 10 μM),增加凋亡[4]
Lactacystin (10μM, 24 h) 增加 Hela 细胞内 Cisplatin (HY-17394) 诱导的内质网应激相关的凋亡[5]
Lactacystin (7.5 μM, 4-48 h) 可提高 HT-29 细胞的活性氧和谷胱甘肽水平[6]
Lactacystin (1, 2.5, 5 μM, 24 h) 诱导新生大鼠皮质星形胶质细胞星性化[7]
Lactacystin (10 μM, 8-24 h) 诱导 PC12 细胞凋亡,G2/M 细胞周期阻滞[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.
体内研究
(In Vivo)

Lactacystin (2 μg, ICV) 在注射后 5-7 天诱导年轻和成年小鼠帕金森病样运动表型[8]
Lactacystin (1.0 ug或5.0µg/20g,连续7天) 导致 C6 原位异种移植肿瘤模型肿瘤明显缩小,并促进组织凋亡[4]
Lactacystin (5 mg/kg/每天,溶解在水中,给药6周) 诱导成年雄性 Wistar 大鼠高血压模型[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 号
性状

固体

颜色

White to off-white

中文名称

蛋白酶体抑制剂

结构分类
初始来源

Streptomyces OM-6519

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 98.08%

参考文献
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  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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