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Cat. No.: HY-189247

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PRDX3-IN-1

PRDX3-IN-1 is an orally active antagonist targeting mitochondrial PRDX3 (K_d=0.514 μM), where PRDX3 is a marker of ferroptosis. PRDX3-IN-1 causes PRDX3 inactivation and disrupts mitochondrial redox homeostasis, inducing apoptosis, ROS accumulation, and a decrease in mitochondrial membrane potential. PRDX3-IN-1 inhibits cell migration and invasion, and downregulates NF-κB and VEGF signaling pathways. PRDX3-IN-1 can be used for research on non-small cell lung cancer.

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

Formula: C₅₅H₆₇BrNO₄P
Molecular Weight:917.00

Storage:

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

PRDX3-IN-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All NF-κB Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
H1975	IC50	0.64 μM	Antiproliferative activity against human H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	42594679
HEK-293T	CC₅₀	0.82 μM	Cytotoxicity against human HEK-293T cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay. Cytotoxicity against human HEK-293T cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.	42594679

In Vitro

PRDX3-IN-1 (0.3-1.2 μM; 15 days) effectively inhibits the clonogenicity of H1975 cells in a concentration-dependent manner^[1].
PRDX3-IN-1 (0.3-1.2 μM; 48 h) significantly inhibits the migration of H1975 cells in a concentration-dependent manner^[1].
PRDX3-IN-1 (0.3-1.2 μM; 48 h) significantly inhibits the invasion of H1975 cells in a concentration-dependent manner^[1].
PRDX3-IN-1 (1 μM; 6 h) effectively accumulates within the mitochondria of H1975 cells^[1].
PRDX3-IN-1 (0.3-1.2 μM; 24 h) induces a dose-dependent decrease in mitochondrial membrane potential in H1975 cells^[1].
PRDX3-IN-1 (Various concentrations; 24 h) inhibits mitochondrial respiration in H1975 cells by reducing basal respiration and ATP production^[1].
PRDX3-IN-1 (0.3-1.2 μM; 24 h) induces a concentration-dependent accumulation of intracellular ROS in H1975 cells^[1].
PRDX3-IN-1 (1.2 μM; 3 h) directly binds to PRDX3 in H1975 cells, as evidenced by increased thermal stability^[1].
PRDX3-IN-1 binds directly and with high affinity to purified PRDX3 protein with a K_d of 0.514 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

H1975
Concentration:

0.3-1.2 μM
Incubation Time:

15 days
Result:

Significantly reduced the number of colonies formed in a concentration-dependent manner.

Cell Migration Assay ^[1]

Cell Line:

H1975
Concentration:

0.3-1.2 μM
Incubation Time:

48 h
Result:

Significantly inhibited H1975 cell migration in a concentration-dependent manner, with inhibition increasing as the concentration increased.

Cell Invasion Assay^[1]

Cell Line:

H1975
Concentration:

0.3-1.2 μM
Incubation Time:

48 h
Result:

Showed a marked reduction in the number of cells that migrated through the membrane.

Immunofluorescence^[1]

Cell Line:

H1975
Concentration:

1 μM
Incubation Time:

6 h
Result:

Accumulated highly within the mitochondria with a Pearson's correlation coefficient of 0.80.

Apoptosis Analysis^[1]

Cell Line:

H1975
Concentration:

Various concentrations
Incubation Time:

48 h
Result:

Increased the total proportion of early and late apoptotic cells progressively with increasing concentration.

Western Blot Analysis^[1]

Cell Line:

H1975
Concentration:

1.2 μM
Incubation Time:

3 h
Result:

Significantly increased the thermal stability of PRDX3.

Parmacokinetics

Species	Dose	Route	T_max	T_1/2	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	F	V_z	CL
Mice^[1]	2 mg/kg	i.v.	0.0833 h	19.9 h	1443 ng/mL	802 ng·h/mL	848 ng·h/mL	1.15 h	3.99 h	/	67766 mL/kg	2360 mL/h/kg
Mice^[1]	10 mg/kg	p.o.	0.194 h	1.51 h	1.66 ng/mL	0.580 ng·h/mL	3.87 ng·h/mL	0.303 h	2.33 h	0.0145 %	/	/

In Vivo

10d (4 mg/kg; i.p.; every other day; 14 days) exhibits significantly superior tumor suppression in a subcutaneous xenograft model of H1975 tumors compared to Celastrol (HY-13067), without causing notable systemic toxicity, and triggers apoptotic cell death in tumors^[1].

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

Animal Model:

BALB/c nude mice (approximately 4-6 weeks old, weighing 20-25 g, subcutaneous xenograft model)^[1]
Dosage:

4 mg/kg
Administration:

i.p.; every other day; 14 days
Result:

Significantly reduced tumor volume and tumor weight compared to control.
Demonstrated superior antitumor effects compared to celastrol at the same dosage.
Showed no significant weight loss.
Exhibited organ architecture and cellular morphology indistinguishable from control with no inflammatory infiltration, necrosis, or degenerative changes.
Showed serum parameters within physiological reference ranges (ALT: 39.94 U/L, AST: 226.87 U/L, UREA: 9.81 mmol/L, CREA: 14.99 μmol/L, UA: 232.84 μmol/L, CK: 1830.38 U/L).
Significantly reduced Ki-67 and VEGF immunoreactivity while robustly increasing Cleaved-Caspase 3 signal intensity in tumor tissues.

Chemical Information

Molecular Weight 917.00
Formula C₅₅H₆₇BrNO₄P
SMILES

O=C(NCC)[C@]1(C)CC[C@]2(C)CC[C@]3(C)C([C@@]4(C)CC[C@@]3(C)[C@]2([H])C1)=CC=C(C4=C5)C(C)=C(OC(CCCCC[P+](C6=CC=CC=C6)(C7=CC=CC=C7)C8=CC=CC=C8)=O)C5=O.[Br-]
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]. Zhao Y, et al. Design, synthesis, and antitumor evaluation of celastrol derivatives targeting PRDX3. European journal of medicinal chemistry. 2026 Aug 10;319:119220.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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