2. NF-κB
  3. NF-κB
  4. Ratutrelvir

Ratutrelvir 是一种 NF-κB p65 抑制剂。Ratutrelvir 可阻断 NF-κB p65 从细胞质向细胞核的转位，降低 NF-κB p65 和 IκBα 的磷酸化水平，并抑制 NF-κB p65 的 DNA 结合活性。Ratutrelvir 可抑制乳腺癌细胞的迁移和侵袭能力，降低其存活率和集落形成能力。Ratutrelvir 可用于管腔 A 型乳腺癌的研究。

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Ratutrelvir

Ratutrelvir Chemical Structure

CAS No. : 2929236-94-0

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Ratutrelvir 相关抗体

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ratutrelvir is a NF-κB p65 inhibitor. Ratutrelvir blocks the translocation of NF-κB p65 from the cytoplasm to the nucleus, reduces the phosphorylation levels of NF-κB p65 and IκBα, and inhibits the DNA-binding activity of NF-κB p65. Ratutrelvir inhibits the migration and invasion abilities of breast cancer cells, and reduces their viability and colony-forming capacity. Ratutrelvir can be used for the research of luminal A breast cancer[1].

体外研究
(In Vitro)

Ratutrelvir (0-100 μM; 24-96 h) 可强效降低 MCF-7 细胞活力，其 IC50 为 53.9 μM；在高浓度下对 MDA-MB-231 和 MCF-10A 细胞仅表现出弱抑制作用，且对 BT474 细胞活力无抑制作用[1]。
Ratutrelvir (0-100 μM; 48 h) 可呈浓度依赖性抑制 MCF-7 细胞集落形成，在 50 μM 浓度下抑制 MDA-MB-231 细胞集落形成，且对 BT474 细胞集落形成无影响[1]。
Ratutrelvir (25 μM; 48 h) 可显著抑制 MCF-7 细胞迁移，但对 MDA-MB-231 或 BT474 细胞的迁移无影响[1]。
Ratutrelvir (12.5 μM; 72 h) 可显著降低 MCF-7 细胞的侵袭能力，但对 MDA-MB-231 或 BT474 细胞的侵袭能力无影响[1]。
Ratutrelvir (0-100 μM; 12 h) 可通过降低 p-NF-κB p65 和 p-IκBα 的水平、阻断 NF-κB p65 的核转位来抑制 MCF-7 细胞中的 NF-κB 通路，但对 MDA-MB-231 或 BT474 细胞中的 NF-κB 通路无影响[1]。
Ratutrelvir (50 μM; 2, 4, 6, 8, 12 h) 可在体外以时间依赖的方式抑制 MCF-7 细胞中 NF-κB 的 DNA 结合活性，但对 MDA-MB-231 或 BT474 细胞的该活性无影响[1]。
Ratutrelvir (0-100 μM; 96 h) 可抑制 MCF-7 细胞中 TNF-α 介导的 NF-κB 激活，且 TNF-α 可部分逆转 Ratutrelvir 对 MCF-7 细胞增殖、迁移及侵袭的抑制作用[1]。

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

Ratutrelvir 相关抗体:

Cell Viability Assay[1]

Cell Line: Human MCF-7, MDA-MB-231, BT474, and MCF-10A breast cells
Concentration: 0, 12.5, 25, 50, 75, 100 μM
Incubation Time: 24, 48, 96 h
Result: Reduced MCF-7 cell viability in a concentration- and time-dependent manner, with an IC50 of 53.9 μM.
Showed a slight inhibitory effect on MDA-MB-231 cells at 75 μM.
Showed no inhibitory effect on BT474 cells at up to 100 μM.
Inhibited MCF-10A cell proliferation only at 75 μM, and this effect was significantly weaker than that on MCF-7 cells.

Cell Proliferation Assay[1]

Cell Line: Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
Concentration: 0, 12.5, 25, 50, 75, 100 μM
Incubation Time: 48 h
Result: Reduced the percentage of surviving MCF-7 cell colonies in a concentration-dependent manner.
Reduced MDA-MB-231 colony formation at 50 μM.
Showed no effect on BT474 colony formation.

Cell Migration Assay [1]

Cell Line: Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
Concentration: 25 μM
Incubation Time: 48 h
Result: Significantly inhibited the migration of MCF-7 cells.
Did not suppress the migration of MDA-MB-231 or BT474 cells.

Cell Invasion Assay[1]

Cell Line: Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
Concentration: 12.5 μM
Incubation Time: 72 h
Result: Significantly reduced the invasiveness of MCF-7 cells.
Did not significantly affect the invasiveness of MDA-MB-231 or BT474 cells.

Western Blot Analysis[1]

Cell Line: Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
Concentration: 0, 25, 50, 75,100 μM (whole-cell lysates); 50 μM (nuclear/cytoplasmic fractionation)
Incubation Time: 12 h
Result: Decreased the expression of p-NF-κB p65 and p-IκBα in a concentration-dependent manner in MCF-7 cells, while NF-κB p65 and IκBα protein levels were not markedly altered.
Notably suppressed the nuclear localization of NF-κB p65 in MCF-7 cells.
Did not alter the levels of p-NF-κB p65, p-IκBα, NF-κB p65, or IκBα in MDA-MB-231 and BT474 cells.
分子量

547.57

Formula

C27H32F3N5O4
CAS 号
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

Ratutrelvir 相关分类

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  • 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:

Ratutrelvir2929236-94-0TRX01TRX 01TRX-01NF-κBNuclear factor-κBNuclear factor-kappaBNF-κB p65 inhibitorbreast cancerMCF-7 cellsMDA-MB-231 cellsBT474 cellsInhibitorinhibitorinhibit

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