For research use only.

Catalog No.S4267

4 publications

Diacerein Chemical Structure

CAS No. 13739-02-1

Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.

Selleck's Diacerein has been cited by 4 publications

1 Customer Review

  • f, Intra-TG injection of IL-1β inhibitor, Diacerein 10 days after pIONL alleviated pIONL-induced mechanical allodynia from 1 to 6 h. *P < 0.05, ***P < 0.001. Two-way repeated measures ANOVA followed by Bonferroni test.

    J Neuroinflammation, 2016, 13(1):183.. Diacerein purchased from Selleck.

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Biological Activity

Description Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
In vitro

Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. Diacerein (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only. Diacerein (1 μM) decreases NO release in synovial tissue and cartilage media and increases IL-1ra levels in cartilage culture media. [1] Diacerein (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes. [2] Diacerein reduces, in a dose-dependent manner, the interleukin-1-beta (IL-1beta)-induced MMP-13 production in osteoarthritic subchondral bone. Diacerein significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. Diacerein effectively blocks the IL-1beta effect on the osteoclast differentiation process and the survival of mature osteoclasts. [3]

Methods Test Index PMID
Western blot
Cyclin B1 / CDK1 / CDK2 ; 

PubMed: 26555773     

Total protein analysis after 48 h of treatment revealed a significant down-regulation of the G2/M arrest regulator proteins cyclin B1, CDK1, and CDK2 in 100 and 300 μM diacerein treated chondrosarcoma cells. β-actin was used as loading control.

AKT / p-AKT / p38 / p-p38 / p53 ; 

PubMed: 26555773     

Western blot analysis confirmed the results of the proteome profiler phospho-MAPK array and showed a significant increase of phospho-Akt and phospho-p38 after the treatment with different concentrations of diacerein in SW-1353 cells, whereas, no significant changes can be observed in the Cal-78 cells. The expression of p53 was diminished in Cal-78 cells.

p-STAT3 / STAT3 ; 

PubMed: 30774444     

H460 cell lines were treated with a concentration gradient of Rhein and Diacerein. The expression of P-STAT3 was found by Western blot analysis. 

MDM2 / CDC2 ; 

PubMed: 30774444     

Western blot analysis of cycle-related proteins MDM2, CDC2, Cyclin B1 and P53 in PC-9.

26555773 30774444
In vivo Diacerein (100 mg/kg/day) significantly suppresses the paw edema and the increase in serum mucoprotein in the adjuvant-induced arthritic rats. Diacerein (30 mg/kg/day) combined with Naproxen (3 mg/kg/day) results in significantly greater anti-inflammatory activity than with naproxen alone in the adjuvant-induced arthritic rats. Diacerein (100 mg/kg/day) also significantly prevents bone loss and reduces the serum alkaline phosphatase and decreases the excretion of urinary hydroxyproline in the ovariectomized rats. [4] Diacerein (25 mg/kg) decreases the thickness of cartilage and subchondral bone in the lesion (middle) zone of the lateral tibial plateau in Merino wethers. [5]


Solubility (25°C)

In vitro DMSO 48 mg/mL (130.33 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 368.29


CAS No. 13739-02-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C2=O)C=C(C=C3OC(=O)C)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03472287 Completed Drug: Diacerein 1% Ointment Epidermolysis Bullosa (EB)|Epidermolysis Bullosa Simplex|Dystrophic Epidermolysis Bullosa|Junctional Epidermolysis Bullosa Castle Creek Pharmaceuticals LLC May 18 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID