1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Apoptosis Reactive Oxygen Species (ROS)
  3. 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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PRDX1-IN-2

PRDX1-IN-2 Chemical Structure

CAS No. : 2566976-43-8

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

PRDX1

0.35 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.44 μM
Compound: 15
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
[PMID: 38679872]
HEK-293T IC50
~ 1 μM
Compound: 15
Antiproliferative activity against HEK293T cells
Antiproliferative activity against HEK293T cells
[PMID: 38679872]
LX-2 IC50
~ 1 μM
Compound: 15
Antiproliferative activity against human LX2 cells
Antiproliferative activity against human LX2 cells
[PMID: 38679872]
SW-620 IC50
0.32 μM
Compound: 15
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
[PMID: 38679872]
In Vitro

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.

Apoptosis Analysis[1]

Cell Line: SW620 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Led to the accumulation of SW620 cells at the G2/M phase with percentages of 7.1−17.4%.

Western Blot Analysis[1]

Cell Line: SW620 cells
Concentration: 0.25-2 μM
Incubation Time: 48 h
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.
In Vivo

PRDX1-IN-2 (20 mg/kg, ip.; everyday for 14 days) possesses superior safety profiles in mice than natural product Celastrol (HY-13067), probably due to its selective PRDX1 inhibitory activity[1].
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

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

Animal Model: C57BL/314 6J mice
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Observed no death or noticeable drop in body weight and no significant pathohistological differences were observed in these key organ tissues.
Animal Model: colorectal cancer cell xenograft model in the BALB/c nude mice
Dosage: 2 mg/kg
Administration: i.g.
Result: Suppressed the tumor volume and weight with the tumor growth inhibition rate (TGI) of 45.4%, which was superior to the group treated with celastrol (TGI = 28.0%).
Molecular Weight

576.77

Formula

C35H48N2O5

CAS No.
SMILES

O=C1C(O)=C(C2=CC=C3[C@](C)([C@]4(CC[C@]3(C2=C1)C)C)CC[C@@]5([C@]4(C[C@](NC(NC6(C(OC)=O)CCC6)=O)(CC5)C)[H])C)C

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

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Product Name:
PRDX1-IN-2
Cat. No.:
HY-158368
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