Peptide R54 acetate  (Synonyms: Pep R54 acetate; CXCR4 antagonist peptide 19 acetate)

Peptide R54 acetate (Pep R54 acetate) is a CXCR4 antagonist. Peptide R54 acetate inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 acetate and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer^[1][2].

Peptide R54 (100 nM; 16 h) acetate significantly inhibits CXCR4-dependent migration toward CXCL12 and CXCL11 in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells^[2].
Peptide R54 (100 nM; 24 h) acetate 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) acetate 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) acetate 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.

Combination treatment with Peptide R54 (2 mg/kg; i.p.; 5 days per week for 3 consecutive weeks) acetate and Nivolumab (HY-P9903) significantly inhibits the growth of PES43 melanoma xenografts^[1].

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

1010.20 (free base)

C₄₄H₆₃N₁₅O₉S₂·xC₂H₄O₂

Ac-Arg-Ala-cyclo{{d-Cys}-Arg-2-Nal-His-Pen}

Ac-RA-cyclo{{d-C}R-2-Nal-H-Pen}

O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@H](CSSC(C)([C@H](NC([C@@H](NC([C@@H](N1)CC(C=C2)=CC3=C2C=CC=C3)=O)CC4=CNC=N4)=O)C(O)=O)C)C(N[C@@H](CCCNC(N)=N)C1=O)=O)=O)=O)C.CC(O)=O.[x]

Room temperature in continental US; may vary elsewhere.

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

• [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]