Peptide R54
Peptide R54 (Pep R54) is a CXCR4 antagonist. Peptide R54 inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 2232233-39-3
- Formula: C44H63N15O9S2
- Molecular Weight:1010.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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CXCR4 |
CXCL12 |
ERK1 |
ERK2 |
In Vitro
Peptide R54 (100 nM; 16 h) significantly inhibits CXCR4-dependent migration toward CXCL12 and CXCL11 in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 24 h) inhibits CXCR4-mediated mesenchymal transition by restoring the expression levels of EMT markers in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 10 min) inhibits CXCR4 downstream signaling pathways by reversing CXCL12-induced phosphorylation of ERK1/2, AKT and p38, as well as reversing the upregulation of RAC1 in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 24-72 h) attenuates CXCL12-induced proliferation and sensitizes CAOV3, OVCAR8 and IGROV1 ovarian cancer cells to cisplatin and paclitaxel[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:16 h
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Result:Reduced the CXCL12-mediated migration index by 2.5-fold in CAOV3 (p<0.01), 2.1-fold in OVCAR8 (p<0.001), and 3-fold in IGROV1 (p<0.01) compared to CXCL12-only treatment.
Reduced the CXCL11-mediated migration index by 3-fold in IGROV1 (p<0.01) and 2-fold in OVCAR8 (p<0.001) compared to CXCL11-only treatment.
Had no impact on migration in CXCR4-knockout IGROV1 cells.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:10 min
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Result:Reversed CXCL12-induced phosphorylation of ERK1/2 and AKT in CAOV3 and OVCAR8; reversed only CXCL12-induced ERK1/2 phosphorylation in IGROV1.
Reversed CXCL12-induced p38 phosphorylation only in OVCAR8.
Reversed CXCL12-induced RAC1 upregulation mainly in IGROV1.
Had no effect on signaling proteins in CXCR4-knockout IGROV1 cells.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:24 h, 48 h, 72 h
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Result:Impaired CXCL12-induced proliferation in all three cell lines.
Reversed CXCL12-induced resistance to cisplatin and paclitaxel, potentiating the growth-inhibiting effects of the chemotherapeutic agents, particularly in OVCAR8 and IGROV1 treated with paclitaxel.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Nude-Foxn1nu mice[1]
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Dosage:2 mg/kg
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Administration:i.p.; 5 days per week; 3 weeks
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Result:Reduced mean tumor volume to 410.33 mm3 compared to untreated controls (622.72 mm3) after 3 weeks of treatment (p = 0.038).
Reduced plasma lactate levels compared to untreated mice (Kruskal Wallis test P = 0.0209).
Showed a non-statistically significant reduction in lung disseminated PES43 tumor cells.
Decreased tumor CXCR4 and PD-L1 (mainly in stromal cells) expression.
Chemical Information
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CAS No. 2232233-39-3
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Molecular Weight 1010.20
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Formula C44H63N15O9S2
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Synonyms
Pep R54; CXCR4 antagonist peptide 19
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Sequence
Ac-Arg-Ala-cyclo{{d-Cys}-Arg-2-Nal-His-Pen}
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Sequence Shortening
Ac-RA-cyclo{{d-C}R-2-Nal-H-Pen}
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. D'Alterio C, et al. Targeting CXCR4 potentiates anti-PD-1 efficacy modifying the tumor microenvironment and inhibiting neoplastic PD-1. J Exp Clin Cancer Res. 2019;38(1):432. Published 2019 Oct 28. [Content Brief]
[2]. Russo D, et al. The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells. PLoS One. 2024;19(12):e0314735. Published 2024 Dec 19. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Peptide R54 Related Classifications
HY-P11011 Related Classifications
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