2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphatase Apoptosis
  4. OA-Br-1

OA-Br-1  (Synonyms: 3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid)

目录号: HY-173165
产品使用指南 技术支持

OA-Br-1 是一种有口服活性的 PTP1B 选择性抑制剂，IC50 值为 7.08 μM。OA-Br-1 诱导细胞凋亡 (apoptosis)。OA-Br-1 具有广谱抗癌细胞增殖活性，通过 PTP1B/PI3K/AKT 信号通路在体内外发挥抗乳腺癌作用。

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OA-Br-1 Chemical Structure

OA-Br-1 Chemical Structure

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Customer Review

OA-Br-1 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

OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo[1].

IC50 & Target

IC50: PTP1B (7.08 μM)[1]
体外研究
(In Vitro)

OA-Br-1 对 PTP1B 有较强的抑制活性，IC50 值为 7.08 μM，对 TCPTP 有较弱的抑制活性，IC50 值为 222.28 μM[1]。
OA-Br-1 (24-72 h) 以浓度和时间依赖性的方式抑制乳腺癌细胞的增殖，72 小时时 MCF-7、MDA-MB-231、MDA-MB-453 的 IC50 值分别为 8.76、18.13、22.34 μM[1]。
OA-Br-1 (5-30 μM; 48 h) 可诱导 MCF-7 和 MDA-MB-231 细胞凋亡[1]。
OA-Br-1 增加了 PTP1B 的热稳定性[1]。
OA-Br-1 (5-30 μM; 48 h) 以剂量依赖性方式减少 MCF-7 和 MDA-MB-231 细胞克隆形成的群落[1]。
OA-Br-1 (5-30 μM; 48 h) 降低 p-PI3K 和 p-AKT 的蛋白水平，表明其通过乳腺癌细胞中的 PTP1B/PI3K/AKT 信号通路发挥抗肿瘤作用[1]。

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

OA-Br-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231
Concentration: 5, 10, 20 μM in MCF-7, 10, 20, 30 μM in MDA-MB-231
Incubation Time: 48 h
Result: The community formed by the two cell clones decreased significantly in dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MCF-7, MDA-MB-231
Concentration: 5, 10, 20, 30 μM
Incubation Time: 48 h
Result: Cells began to show chromatin aggregation, green fluorescence spots, and a few red fluorescence, indicating most cells to enter the early apoptosis stage.
With the continuous increase concentration, the nucleus and chromatin further contracted and aggregated, the proportion of cells with red fluorescence increased, and most cells entered the late apoptotic stage and died.
Induced apoptosis of most breast cancer cells at 20 μM.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10, 20, 30 μM
Incubation Time: 48 h
Result: Inhibited PTP1B protein expression in a concentration-dependent manner in MCF-7 cells.
Decreased the protein levels of p-PI3K and p-AKT.
体内研究
(In Vivo)

OA-Br-1 (30-60 mg/kg；灌胃；每天给药) 通过抑制 PTP1B/PI3K/AKT 信号通路在MCF-7皮下移植BALB/c雌性裸鼠模型中发挥抗肿瘤作用[1]。

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

Animal Model: BALB/c female nude mice (4 weeks old and weighing around 18 g) (5 x 106 MCF-7 cells in 200 μL FBS-free medium were subcutaneously injected into the left axilla)[1]
Dosage: 30, 60 mg/kg
Administration: Intragastric gavage (i.g.); every day
Result: Tumor growth, volume, and weight were inhibited, with no observed toxicity on body weight or major organ weight indices.
Suppressed the expression of PTP1B, as well as the phosphorylation level of PI3K and AKT protein in the tumor.
分子量

808.92

Formula

C43H70BrNO8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

OA-Br-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

OA-Br-13-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acidPhosphataseApoptosisbreast cancerMCF-7MDA-MB-231PTP1B inhibitorInhibitorinhibitorinhibit

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