RR-171
RR-171 is an amino acid polypeptide and an inhibitor of the Wnt signaling pathway. RR-171 reduces the expression levels of Wnt-1, GSK3β and β-catenin. RR-171 induces apoptosis (Apoptosis) in pancreatic cancer cells, which is characterized by an increased Bax/Bcl-2 ratio, activation of Caspase-3/7/9, and increased Cleaved-PARP; this pro-apoptotic effect can be partially reversed by Z-VAD-FMK (HY-16658B). RR-171 also induces pyroptosis (Pyroptosis) in pancreatic cancer cells, which is manifested by activation of the NLRP-3 inflammasome, activation of Caspase-1, cleavage of GSDMD, upregulation of IL-1β and IL-18, and increased LDH release; this pro-pyroptotic effect can be partially reversed by VX-765 (HY-13205). RR-171 inhibits the viability, proliferation and colony formation of pancreatic cancer cells, with low cytotoxicity against normal cells. RR-171 downregulates the expression of Ki-67 and PCNA in tumor tissues in vivo, with favorable biosafety. RR-171 can be used in studies related to pancreatic cancer.
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- CAS. Nr.: 2410535-57-6
- Formel: C92H177N41O18
- Molecular Weight:2145.65
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Speicherung:
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Biologische Aktivität
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Caspase-1 |
Caspase-3 |
Caspase-9 |
Caspase-7 |
IL-1β |
IL-18 |
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Cell Line
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Type | Value | Description | References |
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| Capan-2 | IC50 |
24.70 μM
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Inhibition of cell viability against human Capan-2 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human Capan-2 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
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40229415 |
| BXPC-3 | IC50 |
15.71 μM
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Inhibition of cell viability against human Bxpc-3 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human Bxpc-3 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
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40229415 |
| PANC-1 | IC50 |
75.68 μM
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Inhibition of cell viability against human Panc-1 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human Panc-1 pancreatic cancer cells incubated for 24 hrs by CCK-8 assay.
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40229415 |
RR-171 (0-200 µM; 24 h) inhibits the viability of Panc-1, Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner, with IC50 values of 75.68 µM, 24.70 µM and 15.71 µM, respectively; whereas it exerts weak inhibitory effects on HPNE normal pancreatic epithelial cells (IC50 = 144.50 µM)[1].
RR-171 (0-20 µM; 24 h) inhibits colony formation of Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner[1].
RR-171 (0-20 µM; 48 h) inhibits the proliferation of Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner[1].
RR-171 (0-20 µM; 24 h) reduces the expression of Wnt-1, GSK3β and β-catenin in Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner, thereby inhibiting the canonical Wnt signaling pathway[1].
RR-171 (0-20 µM; 24 h) regulates the expression of apoptosis-related proteins in Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner; it increases the levels of Bax and cleaved PARP, while decreasing the levels of Bcl-2, caspase-3, caspase-7 and caspase-9[1].
Treatment of Capan-2 pancreatic cancer cells with RR-171 (20 µM; 24 h) alters their global gene expression, thereby enriching apoptosis-related pathways and inhibiting the canonical Wnt signaling pathway[1].
RR-171 (0-20 µM; 24 h) induces caspase-mediated apoptosis in Capan-2 and Bxpc-3 pancreatic cancer cells in a dose-dependent manner, and this effect is partially reversed by Z-VAD-FMK (HY-16658B)[1].
Treatment of Capan-2 pancreatic cancer cells with RR-171 (5-20 µM; 24 h) induces dose-dependent morphological changes consistent with pyroptosis, including reduced cell junctions, membrane blebbing and cell rupture[1].
RR-171 (0-20 µM; 24 h) induces dose-dependent LDH release in Capan-2 and Bxpc-3 pancreatic cancer cells. This effect is significantly reversed by the pyroptosis inhibitor VX-765, but cannot be completely reversed by the pan-caspase inhibitor Z-VAD-FMK[1].
RR-171 (0-20 µM; 24 h) dose-dependently upregulates the expression of pyroptosis-related proteins (NLRP-3, GSDMD, caspase-1, IL-1β, IL-18) in Capan-2 and Bxpc-3 pancreatic cancer cells, and this effect is reversed by VX-765 (HY-13205)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc-1, Capan-2, Bxpc-3, HPNE
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Concentration:0, 0.5, 1, 5, 10, 20, 40, 80, 100 and 200 µM
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Incubation Time:24 h
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Result:Inhibited pancreatic cancer cell viability in a dose-dependent manner, with reduced inhibitory effects on normal pancreatic epithelial cells.
Achieved IC50 values of 24.70 µM for Capan-2 cells, 15.71 µM for Bxpc-3 cells, 5075.68 µM for Panc-1 cells, and 144.50 µM for HPNE cells at 24 h.
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Cell Line:Capan-2, Bxpc-3
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Concentration:5, 10 and 20 µM
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Incubation Time:48 h
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Result:Distinctly suppressed the proliferation of Capan-2 and Bxpc-3 cells in a dose-dependent manner, as indicated by reduced EdU-positive staining relative to control cells.
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Cell Line:Capan-2, Bxpc-3
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Concentration:5, 10 and 20 µM
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Incubation Time:24 h
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Result:Decreased the expression levels of Wnt-1, GSK3β, and β-catenin in a dose-dependent manner in both Capan-2 and Bxpc-3 cells, confirming inhibition of the canonical Wnt signaling pathway.\nDecreased antiapoptotic protein Bcl-2 expression, while increased proapoptotic protein Bax expression in a dose-dependent manner as concentration increased.
Reduced levels of caspase-3, caspase-7, and caspase-9, while increased cleaved-PARP levels, indicating activation of the caspase-mediated apoptosis pathway.
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Cell Line:Capan-2, Bxpc-3
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Concentration:5, 10 and 20 µM
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Incubation Time:24 h
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Result:Distinctively increased the percentage of apoptotic Capan-2 and Bxpc-3 cells in a dose-dependent manner.
Significantly reduced the apoptosis ratio in both cell lines when co-treated with Z-VAD-FMK, confirming a caspase-dependent mechanism.
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Cell Line:Capan-2, Bxpc-3
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Concentration:5, 10 and 20 µM
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Incubation Time:24 h
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Result:Increased levels of NLRP-3, GSDMD, caspase-1, IL-1β, and IL-18 in a dose-dependent manner in both cell lines.
Decreased the elevated levels of these pyroptosis-related proteins when co-treated with VX-765.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 5-6 weeks old, subcutaneous pancreatic cancer xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; every 3 days; three weeks
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Result:Reduced tumor volume significantly starting on Day 17 post-cell injection.
Lowered final tumor weight significantly compared to controls.
Showed no significant difference in mouse body weight between groups.
Decreased average density of Ki-67 and PCNA in tumor tissues significantly.
Exhibited no significant organ toxicity in lung, heart, liver, spleen, and kidney tissues.
Chemical Information
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CAS. Nr. 2410535-57-6
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Molecular Weight 2145.65
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Formel C92H177N41O18
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Sequence
Arg-Arg-Arg-Arg-Leu-Val-Ala-Gly-Val-Leu-Val-Leu-Leu-Arg-Arg-Arg-Arg
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Sequence Shortening
RRRRLVAGVLVLLRRRR
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RR-171 Related Classifications
HY-P11935 Related Classifications
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