2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK Apoptosis NF-κB Immunology/Inflammation
  3. Proteasome VEGFR Apoptosis Reactive Oxygen Species (ROS)
  4. MG-262

MG-262  (Synonyms: Z-Leu-Leu-LeuB(OH)2; ZL3B)

目录号: HY-108551 纯度: ≥95.0%
COA 产品使用指南 技术支持

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) 是一种可逆性蛋白酶体 (proteasome) 抑制剂。MG-262 下调 VEGF 受体 Flt-1。MG-262 可抑制恶性细胞生长并诱导细胞凋亡 (apoptosis)。MG-262 诱导活性氧 (ROS)。MG-262 可用于癌症研究。

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MG-262 Chemical Structure

MG-262 Chemical Structure

CAS No. : 179324-22-2

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MG-262 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study[1][2][3][4][5].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
5TGM1 IC50
9.18 nM
Compound: MG-262
Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay
Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay
[PMID: 24119559]
RPMI-8226 IC50
13.76 nM
Compound: MG-262
Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay
Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay
[PMID: 24119559]
体外研究
(In Vitro)

MG-262 (1 μM，16 小时) 下调鸡眼梳膜外植体中 VEGF 受体 Flt-1 (血管内皮生长因子受体 1) 的基因表达[1]。
MG-262 (500 nM，12 小时) 下调人类微血管内皮细胞中的 Flt-1 基因表达[1]。
MG-262 (500 nM，12 小时) 可抑制巨噬细胞中 Lipopolysaccharide (LPS) (HY-D1056) 诱导的 Flt-1，并在 LPS 诱导后下调 Flt-1 的表达[1]。
MG-262 (0.1 nM-1 μM，24 h) 在 HEK293 细胞中以浓度依赖性方式增加 IL-8 启动子和激活蛋白-1 (AP-1) 的活性，但抑制细胞因子诱导的 NF-κB 活化 (IC50 = 1-3 nM)[2]。
MG-262 (0.1 μM，5-180 min) 以时间依赖性方式增加 HEK293 细胞内的活性氧[2]。
MG262 (0.125-1 μM，48 h) 抑制 H22 和 K562 细胞的生长，并与 Gambogic Acid (GA) (HY-N0087) 联合具有协同作用。[3]。
MG262 (0.025 μM，24 h) 与 GA 联合使用可诱导 H22 和 K562 细胞凋亡[3]。
MG262 (0.025 μM，12 或 24 h) 与 GA 联合使用可诱导 K562 细胞中 PARP 裂解以及 caspase 8 和 9 裂解/活化，但单独使用时则不会产生这种效果[3]。

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

MG-262 相关抗体:

Cell Viability Assay[3]

Cell Line: Murine hepatoma H22 and human leukemia K562 cells
Concentration: 0.125, 0.25, 0.5, 1 μM
Incubation Time: 48 h
Result: From 5% when treated with 6.25 nM alone to 82% when combined with GA in K562 cells.
The addition of GA boosted the inhibitory effects on cell viability/proliferation from 11% to 73%.

Apoptosis Analysis[3]

Cell Line: Murine hepatoma H22 and human leukemia K562 cells
Concentration: 0.025 μM
Incubation Time: 24 h
Result: Showed that co-treatment of these malignant cells, especially K562 cells, dramatically increased the population of both Annexin V and propidium iodide (PI) stained cells, indicating that the combination with GA induced more cell death than each alone.

RT-PCR[1]

Cell Line: explant cultures of whole pecten oculi
Concentration: 1 μM
Incubation Time: 16 h
Result: The level of Flt-1 transcripts markedly decreased in the presence of the proteasome inhibitor.
The level of the KDR, VEGF, Ang-1 and Ang-2 transcripts was not changed by the presence of the proteasome inhibitor.

RT-PCR[1]

Cell Line: Human microvascular dermal neonatal endothelial cells (HMVEC-d-Neo)
Concentration: 500 nM
Incubation Time: 12 h
Result: The level of Flt-1 transcripts markedly decreased in the presence of the proteasome inhibitor.

Western Blot Analysis[3]

Cell Line: K562 cells
Concentration: 25 nM
Incubation Time: 12 or 24 h
Result: The GA + proteasome inhibitor, but not GA or proteasome inhibitor alone, could induce cleavage of PARP as well as cleavage/activation of caspases 8 and 9.
体内研究
(In Vivo)

MG-262 (5 μmol/kg (2.5 mg/kg)；静脉注射；收集组织样本前 20 小时) 使 GFPdgn 转基因小鼠中的 GFPdgn 蛋白积累[4]。
MG-262 (1-5 μmol/kg (0.5-2.5 mg/kg)；腹腔注射；测试前 20 小时) 会在 UbG76V-GFP/1 小鼠肝脏中积聚 GFP 报告基因，表明泛素/蛋白酶体系统受到严重损害[5]。

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

Animal Model: UbG76V-GFP/1 mice (The transgenic construct was injected into fertilized CBA × C57BL/6 F1 oocytes. Transgenic founders were backcrossed to C57BL/6 mice)[5]
Dosage: 1, 5 μmol/kg (0.5, 2.5 mg/kg)
Administration: Intraperitoneal injection (i.p.); 20 h before test
Result: Fluorescent cells were detected exclusively in the livers, resulted in accumulation of GFP in the vast majority of hepatocytes distributed throughout the live.
A dose-dependent decrease of the chymotrypsin-like activity of the proteasome was observed in lysates of the liver, kidney and spleen.
Animal Model: Transgenic mice (ubiquitously expresses a surrogate protein substrate for the Ubiquitin-proteasome system, referred to as GFPdgn)[4]
Dosage: 5 μmol/kg (2.5 mg/kg)
Administration: Intravenous injection (i.v.); 20 h before the tissue samples were collected
Result: Inhibited chymotryptic activity in the heart, lungs, skeletal (Sk.) muscle, and liver by 50-75%.
GFPdgn levels in all the indicated organs clearly displayed significant increases.
分子量

491.43

Formula

C25H42BN3O6
CAS 号
性状

固体

颜色

White to off-white

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 : 5 mg/mL (10.17 mM; 超声助溶; 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 2.0349 mL 10.1744 mL 20.3488 mL
5 mM 0.4070 mL 2.0349 mL 4.0698 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: ≥95.0%

COA (268 KB)

产品使用指南 (1538 KB)
参考文献

MG-262 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 2.0349 mL 10.1744 mL 20.3488 mL 50.8719 mL
5 mM 0.4070 mL 2.0349 mL 4.0698 mL 10.1744 mL
10 mM 0.2035 mL 1.0174 mL 2.0349 mL 5.0872 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:

MG-262179324-22-2Z-Leu-Leu-LeuB(OH)2 ZL3BMG262MG 262ProteasomeVEGFRApoptosisReactive Oxygen Species (ROS)Vascular endothelial growth factor receptoranti-cancerH22 cellsK562 cellsubiquitinangiogenesismicrovascular endothelial cellsInhibitorinhibitorinhibit

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