1. NF-κB
  2. NF-κB
  3. Ratutrelvir

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.

For research use only. We do not sell to patients.

Ratutrelvir

Ratutrelvir Chemical Structure

CAS No. : 2929236-94-0

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Description

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].

In Vitro

Ratutrelvir (0-100 μM; 24-96 h) potently reduces the viability of MCF-7 cells, with an IC50 of 53.9 μM; it only exerts weak inhibitory effects on MDA-MB-231 and MCF-10A cells at high concentrations, and shows no inhibitory effect on the viability of BT474 cells[1].
Ratutrelvir (0-100 μM; 48 h) inhibits colony formation of MCF-7 cells in a concentration-dependent manner, suppresses colony formation of MDA-MB-231 cells at a concentration of 50 μM, and exerts no effect on colony formation of BT474 cells[1].
Ratutrelvir (25 μM; 48 h) significantly inhibits the migration of MCF-7 cells, but exerts no effect on the migration of MDA-MB-231 or BT474 cells[1].
Ratutrelvir (12.5 μM; 72 h) significantly reduces the invasive ability of MCF-7 cells, but exerts no effect on the invasive ability of MDA-MB-231 or BT474 cells[1].
Ratutrelvir (0-100 μM; 12 h) inhibits the NF-κB pathway in MCF-7 cells by reducing the levels of p-NF-κB p65 and p-IκBα and blocking the nuclear translocation of NF-κB p65, but exerts no effect on the NF-κB pathway in MDA-MB-231 or BT474 cells[1].
Ratutrelvir (50 μM; 2, 4, 6, 8, 12 h) inhibits the DNA-binding activity of NF-κB in MCF-7 cells in a time-dependent manner in vitro, but exerts no effect on this activity in MDA-MB-231 or BT474 cells[1].
Ratutrelvir (0-100 μM; 96 h) inhibits TNF-α-mediated NF-κB activation in MCF-7 cells, and TNF-α can partially reverse the inhibitory effects of Ratutrelvir on the proliferation, migration and invasion of MCF-7 cells[1].

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

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.
Molecular Weight

547.57

Formula

C27H32F3N5O4

CAS No.
SMILES

CC1(C)[C@](CN2C([C@H](C(C)(C)C)NC(C(F)(F)F)=O)=O)([H])[C@@]1([H])[C@H]2C(N[C@@H](CC3C(NC4=CC=CC=C43)=O)C#N)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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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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Ratutrelvir
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