R9-caPep
R9-caPep (RRRRRRRRRCCLGIPEQEY) is a cell-penetrating peptide derived from proliferating cell nuclear antigen (PCNA). R9-caPep selectively blocks the interactions between PCNA and FEN1, as well as between PCNA and LIGI, while preserving the binding of POLD3 to PCNA. R9-caPep interferes with DNA synthesis and homologous recombination-mediated double-strand DNA break repair, inducing S-phase arrest, DNA damage accumulation, and apoptosis. R9-caPep inhibits the growth of tumor volume and weight of neuroblastoma in nude mice. R9-caPep can be used in research related to neuroblastoma and triple-negative breast cancer.
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- CAS No.: 1207092-73-6
- Formule: C103H183N47O26S2
- Masse moléculaire:2560.02
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
R9-caPep (72 h) inhibits the proliferation of various neuroblastoma cell lines, with an IC50 ranging from 10 to 32 mM, and blocks the interaction of proliferating cell nuclear antigen (PCNA)[1].
R9-caPep (0-40 μM, 72 h) significantly reduces the proportion of bromodeoxyuridine-positive cells in SK-N-BE (2) c cells, causes cell DNA replication arrest, inhibits SV40T antigen-mediated DNA replication, induces S-phase cell cycle arrest, and triggers cell apoptosis[1].
R9-caPep (60 μM; 72 h) induces cell death in most tested breast cancer cell lines, with the strongest effects observed in HCC1428 cells (49% increase in cell death) and MDA-MB-231 cells (47% increase in cell death), while exerting no significant effect on BT474 cells[2].
R9-caPep (75 μM, 0-72 h) induces progressive DNA damage and apoptosis in MDA-MB-231 cells. The level of γH2AX increases continuously starting at 24 h, and more than 70% of cells exhibit PARP cleavage by 72 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-BE(2)c cells
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Concentration:0, 20, 40 μM
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Incubation Time:48 h
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Result:Caused S-phase cell cycle arrest in neuroblastoma cells, and increased the proportion of cells in the sub-G1 phase.
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Cell Line:HCC1428, MDA-MB-231, BT474, MDA-MB-436, MCF7, SKBR3, MDA-MB-468, HCC1143, HCC1937, UACC893, HCC38, MDA-MB-361, HCC1569
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Concentration:60 μM
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Incubation Time:72 h
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Result:Induced increased cell death relative to scrambled control in all tested breast cancer cell lines except BT474.
Increased cell death by 49% in HCC1428 cells.
Increased cell death by 47% in MDA-MB-231 cells.
Showed no significant cell death increase in BT474 cells.
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Cell Line:MDA-MB-231
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Concentration:75 μM
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Incubation Time:12, 24, 48, 72 h
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Result:Increased the population of cells with high γH2AX levels over the first 24 h, with levels remaining elevated through 72 h.
Increased the percentage of cells with high levels of cleaved PARP progressively over 72 h, rising from 0.2% at 0 h to over 70% by 72 h.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (6 weeks, SK-N-BE(2)c cells (5x107 xenografts)) [1]
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Dosage:/
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Administration:intratumoral injection, three times per week
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Result:Inhibited the growth of tumor volume and mass of neuroblastoma in nude mouse xenograft models.
Chemical Information
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CAS No. 1207092-73-6
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Masse moléculaire 2560.02
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Formule C103H183N47O26S2
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Synonyms
RRRRRRRRRCCLGIPEQEY
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Sequence
Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Cys-Leu-Gly-Ile-Pro-Glu-Gln-Glu-Tyr
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Sequence Shortening
RRRRRRRRRCCLGIPEQEY
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Gu L, et al. A PCNA-derived cell permeable peptide selectively inhibits neuroblastoma cell growth. PLoS One. 2014;9(4):e94773. Published 2014 Apr 11. [Content Brief]
[2]. Lingeman RG, et al. Expression of a novel peptide derived from PCNA damages DNA and reverses cisplatin resistance. Cancer Chemother Pharmacol. 2014;74(5):981-993. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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