2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species (ROS) NOD-like Receptor (NLR)
  4. PRDX1-IN-4

PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis.

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PRDX1-IN-4

PRDX1-IN-4 Chemical Structure

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PRDX1-IN-4 Related Antibodies

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Description

PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis[1].

IC50 & Target

NLRP3

 

In Vitro

PRDX1-IN-4 (derivative 5) (0.1-2 μM; 48 h treatment) dose-dependently reduces the protein expression levels of α-SMA and COL1A1 in TGF-β1-induced activated LX-2 cells[1].
PRDX1-IN-4 (0.1-2 μM; 48 h treatment) dose-dependently increases TGF-β1-induced intracellular ROS levels in activated LX-2 cells, with ROS positive rates reaching 18.0%, 26.4% and 34.7% at concentrations of 0.1, 1 and 2 μM, respectively[1].
PRDX1-IN-4 (0.1-1 μM; 48 h treatment) dose-dependently upregulates the expression of pro-apoptotic proteins Bax, Cyt c, and activated Caspase-3, and downregulates the expression of anti-apoptotic protein Bcl-2 and pro-Caspase-3 in TGF-β1-induced activated LX-2 cells[1].
PRDX1-IN-4 (0.5 μM; 6 h) exerts no significant effect on the viability of THP-M cells, and its NLRP3 inhibitory activity is not derived from cytotoxicity[1].

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

PRDX1-IN-4 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: THP-1-derived macrophages (induced by 100 ng/mL PMA overnight)
Concentration: 0.5 μM
Incubation Time: 6 h
Result: Showed no significant effect on the viability of THP-M cells, indicating that its NLRP3 inhibitory activity was not attributed to cytotoxicity.

Western Blot Analysis[1]

Cell Line: THP-1-derived macrophages (induced by 100 ng/mL PMA overnight)
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: Pretreated for 0.5 h, then stimulated with 10 μM Nigericin for 1 h, 5 mM ATP for 1 h, or 200 μg/mL MSU for 4 h
Result: Dose-dependently reduced the levels of cleaved caspase-1 p20 and mature IL-1β in the supernatants, and inhibited ASC oligomerization in the pellets. It did not consistently affect the expression of pro-IL-1β, pro-caspase-1, total ASC, or NLRP3 in the cell lysates.
In Vivo

PRDX1-IN-4 (derivative 5) (20 mg/kg; i.p.; single administration; 14-day observation period) causes no mortality in the acute toxicity model of wild-type male C57BL/6 mice. It induces no significant body weight loss or histopathological damage in the heart, liver, spleen, lung or kidney, and no abnormalities in serum ALT, AST levels or red blood cell counts. Its safety is significantly superior to that of celastrol at the same dose[1].
PRDX1-IN-4 (1 mg/kg; intraperitoneal injection; once daily for 4 consecutive weeks, starting from the 3rd week of modeling) significantly ameliorates CCl4-induced liver injury and fibrosis in the CCl4-induced hepatic fibrosis model of male C57BL/6 mice. It reduces the liver/body weight ratio, serum ALT and AST levels, and collagen fiber deposition, downregulates the expressions of α-SMA and COL1A1 in liver tissues, and inhibits NLRP3 inflammasome activation. No mouse death is observed, and its safety is superior to that of celastrol at the same dose[1].

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

Animal Model: Male C57BL/6 mice, housed under SPF conditions, acclimatized for 1 week; hepatic fibrosis model established by intraperitoneal injection of CCl4 (1 mL/kg, diluted 1:8 in corn oil) twice weekly for 6 consecutive weeks[1]
Dosage: 1 mg/kg
Administration: intraperitoneal injection once daily for 4 weeks
Result: Significantly normalized the liver/body weight ratio and reduced the serum levels of ALT and AST, indicating improved liver function. H&E staining showed that derivative 5 alleviated CCl4-induced hemorrhagic necrosis and inflammatory cell infiltration in the liver.
Markedly reduced collagen fiber deposition in the fibrotic liver.
Downregulated the protein expression of α-SMA and COL1A1, and decreased the levels of IL-1β and cleaved caspase-1 without altering the total expression of NLRP3.
Molecular Weight

629.62

Formula

C33H45BrN2O5
SMILES

C[C@@H](C(OC)=O)NC(N[C@@](CC[C@]1(C)CC[C@]2(C)C3=CC=C4C(C)=C5O)(C)C[C@@]1([H])[C@]2(C)C[C@@](Br)([H])[C@@]3(C)C4=CC5=O)=O
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Purity & Documentation
References
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PRDX1-IN-4 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-4Reactive Oxygen Species (ROS)NOD-like Receptor (NLR)hepatotoxicitymiceapoptosishepatic fibrosishepatic stellate cellcollagen depositionNLRP3 inflammasomePRDX1ROSCCl4-induced hepatic damageInhibitorinhibitorinhibit

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