PRDX1-IN-2
PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) (IC50=0.35 μM). PRDX1-IN-2 decreases the mitochondria membrane potential of SW620 cells, probably due to ROS induced by PRDX1 inhibition, leading to cell apoptosis. PRDX1-IN-2 can be used for colorectal cancer research.
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- CAS No.: 2566976-43-8
- Formule: C35H48N2O5
- Masse moléculaire:576.77
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Activité biologique
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Activité biologique
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PRDX1 0.35 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.44 μM
Compound: 15
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Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay
Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38679872] |
| HEK-293T | IC50 |
~ 1 μM
Compound: 15
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Antiproliferative activity against HEK293T cells
Antiproliferative activity against HEK293T cells
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[PMID: 38679872] |
| LX-2 | IC50 |
~ 1 μM
Compound: 15
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Antiproliferative activity against human LX2 cells
Antiproliferative activity against human LX2 cells
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[PMID: 38679872] |
| SW-620 | IC50 |
0.32 μM
Compound: 15
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Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay
Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38679872] |
PRDX1-IN-2 (0.5-2 μM, 48 h) increases ROS levels in a dose-dependent manner[1].
PRDX1-IN-2 could induce depolarization of the mitochondrial membrane and decrease mitochondrial membrane potential, thus eventually leading to mitochondrial dysfunction[1].
PRDX1-IN-2 (0.5, 1, 2 μM, 48 h) induces the apoptosis of colon cancer cells and G2/M cell cycle arrest, which might contribute to its antiproliferative activity[1].
PRDX1-IN-2 (0.25-2 μM, 48 h) induces apoptosis of SW620 by regulating pro- or antiapoptotic marker proteins that is related to the mitochondrial dysfunction, which eventually leads to the antiproliferation phenotype[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Led to the accumulation of SW620 cells at the G2/M phase with percentages of 7.1−17.4%.
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Cell Line:SW620 cells
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Concentration:0.25-2 μM
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Incubation Time:48 h
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Result:Increased the expression of Cyt C, down-regulated the expression of anti-apoptotic proteins Bcl-2 and Bcl-xL, and accumulated the DNA damage marker γ-h2ax in a dose-dependent manner.
PRDX1-IN-2 (2 mg/kg, ig.; once a day for 16 days) successfully inhibits tumor growth in vivo through the induction of cell apoptosis with well tolerance in colorectal cancer cell xenograft model[1].
Pharmacokinetic Analysis in C57BL/314 6J mice[1]
| Route | Dose (mg/kg) | AUC0_t (ng•h/mL) | AUC0_INF (ng•h/mL) | T1/2 (h) | Cmax (ng/mL) | Cl (L•h/kg) | V2(mL/kg) |
| i.v. | 2 | 364 | 403 | 8.46 | 203 | 4986 | 60699 |