PRDX1-IN-2

Cat. No.: HY-158368: FAQs
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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.

For research use only. We do not sell to patients.

PRDX1-IN-2 Chemical Structure

CAS No. : 2566976-43-8

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Description

IC₅₀ & Target

PRDX1

0.35 μM (IC₅₀)

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)	AUC_{0_t} (ng•h/mL)	AUC_{0_INF} (ng•h/mL)	T_1/2 (h)	C_max (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.

2566976-43-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells[J]. Journal of Medicinal Chemistry, 2024. [Content Brief]

PRDX1-IN-2 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRDX1-IN-22566976-43-8ApoptosisROS KinaseROScolorectal cancerPRDX1C57BL/314 6J miceSW620 cellsInhibitorinhibitorinhibit

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