2. 诱导疾病模型产品 Metabolic Enzyme/Protease Apoptosis Protein Tyrosine Kinase/RTK
  3. 神经系统疾病模型 Proteasome Apoptosis ROS Kinase
  4. 帕金森综合症模型
  5. Lactacystin

Lactacystin  (Synonyms: 蛋白酶体抑制剂)

目录号: HY-16594 纯度: 98.20%
COA 产品使用指南 技术支持

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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Lactacystin 相关抗体

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DLD-1 IC50
0.07 μM
Compound: Lactacystin
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
[PMID: 22206869]
DLD-1 IC50
0.3 μM
Compound: Lactacystin
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
[PMID: 22206869]
MDA-MB-468 IC50
0.37 μM
Compound: Lactacystin
Inhibition of chymotrypsin-like activity of proteasome beta5 subunit in human MDA-MB-468 cells using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 2 hrs by fluorescence assay
Inhibition of chymotrypsin-like activity of proteasome beta5 subunit in human MDA-MB-468 cells using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 2 hrs by fluorescence assay
[PMID: 23547706]
NCI-H23 IC50
5.23 μM
Compound: Lactacystin
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
[PMID: 30964987]
NCI-H727 IC50
> 100 μM
Compound: Lactacystin
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
[PMID: 30964987]
U-251 IC50
3481 nM
Compound: 4
Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
[PMID: 17643112]
体外研究
(In Vitro)

Lactacystin (up to 25.6 µM, 1 h) has no cytotoxicity to HeLa or SH-SY5Y cells, and decreases RVP infection by 63.8% in HeLa and by 74.5% in SH-SY5Y cells[2].
Lactacystin (2.5 μM) in combination with Parthenolide (HY-N0141) (5 μM) causes a synergistic increase in the apoptotic fraction of the drug-resistant L1210 cells[3].
Lactacystin（2.5, 5 and 10  µM, 24 h）inhibits the proliferation (IC50 value of 10 μ M) and increases the apoptotic in C6 cells[4].
Lactacystin (10μM, 24 h) increases Cisplatin (HY-17394)-induced ER stress-associated apoptosis in Hela cells[5].
Lactacystin (7.5 μM, 4-48 h) increased reactive oxygen species and GSH levels in HT-29 cells[6].
Lactacystin (1, 2.5, 5 μM, 24 h) induces stellation in astrocytes from neonatal rat cortex[7].
Lactacystin (10μM, 8-24 h) induces apoptosis, G2/M cell cycle arrest in the PC12 cells[10].

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

Lactacystin 相关抗体:

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 (显微注射; 2 μg) 在年轻和成年小鼠注射 5-7 天后诱导帕金森病样运动表型[2]。

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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 20 mg/mL (53.13 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.20%

COA (294 KB)

产品使用指南 (1538 KB)
参考文献

Lactacystin 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

Keywords:

Lactacystin133343-34-7蛋白酶体抑制剂ProteasomeApoptosisROS KinaseL1210C6HelaSHSY-5YHT-29Parkinson’s diseasehypertensionMalariaantiviralanticancerantioxidativeInhibitorinhibitorinhibit

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