1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. PDI
  3. Dicentrinone

Dicentrinone is an orally active PDI inhibitor with an IC50 value of 43.95 μM. Dicentrinone directly binds to PDI and suppresses cell proliferation and reduces cancer cell viability. Dicentrinone elicits anti-inflammatory and antioxidant effects by suppressing leukocyte migration, plasma leakage and paw edema, and scavenging free radicals. Dicentrinone can be used in the research of hepatoma, rheumatism and arthritis.

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

Dicentrinone

Dicentrinone Chemical Structure

CAS No. : 16408-78-9

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Description

Dicentrinone is an orally active PDI inhibitor with an IC50 value of 43.95 μM. Dicentrinone directly binds to PDI and suppresses cell proliferation and reduces cancer cell viability. Dicentrinone elicits anti-inflammatory and antioxidant effects by suppressing leukocyte migration, plasma leakage and paw edema, and scavenging free radicals. Dicentrinone can be used in the research of hepatoma, rheumatism and arthritis[1][2][3].

In Vitro

Dicentrinone (compound 1) (1-100 μM; 48 h) potently suppresses HepG2 cell proliferation with a CC50 of 20.70 μM[1].
Dicentrinone (3-300 μM; 1 h) inhibits purified bovine PDI activity with an IC50 of 56.70 μM[1].
Dicentrinone (56.70 μM; 48 h) suppresses HepG2 cell viability specifically through inhibition of PDI, as co-treatment with PDI siRNA does not enhance its cytotoxic effect[1].
Dicentrinone (72 h) does not inhibit the growth of MCF-7, HCT116, HepG2, HL-60, or MRC-5 cells, with IC50 >10 μM[2].

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

Cell Proliferation Assay[1]

Cell Line: human hepatoma HepG2 cells
Concentration: log0, log0.5, log1, log1.5, log2 μM
Incubation Time: 48 h
Result: Reduced HepG2 cell viability in a dose-dependent manner: at 1 μM, cell viability was 75.29%; at 10 μM, cell viability was 59.98%; at 50 μM, cell viability was 11.79%.
Calculated the 50% cytotoxic concentration (CC50) as 20.70 μM.

Cell Viability Assay[1]

Cell Line: human hepatoma HepG2 cells
Concentration: 56.70 μM
Incubation Time: 48 h (siRNA transfection prior to treatment)
Result: Reduced the cell number index to 0.54 in the siCtl group compared to untreated siCtl cells.
Showed no further reduction of cell number index when co-treated with siPDI compared to siPDI alone.
In Vivo

Dicentrinone (100 mg/kg; p.o.) significantly inhibits Carrageenan-induced paw edema in Swiss mice at both 2 and 4 hours post-induction[3].
Dicentrinone (100 mg/kg; p.o.) inhibits Carrageenan-induced leukocyte migration by 69.1% and plasma leakage by 50.4% in the Swiss mouse air pouch inflammation model[3].
Dicentrinone (100 mg/kg; p.o.) significantly inhibits zymosan-induced leukocyte recruitment and articular edema in male mice via intra-articular induction[3].

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

Molecular Weight

335.31

Formula

C19H13NO5

CAS No.
SMILES

O=C1C2=NC=CC3=CC4=C(C(C5=C1C=C(OC)C(OC)=C5)=C23)OCO4

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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.

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Dicentrinone
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HY-N19464
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