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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CXCR4 |
CXCL12 |
ERK1 |
ERK2 |
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.
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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