Catalog No.S4267

For research use only.

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

Diacerein Chemical Structure

CAS No. 13739-02-1

Selleck's Diacerein has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Interleukins Inhibitors

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 ; AKT / p-AKT / p38 / p-p38 / p53 ; p-STAT3 / STAT3 ; MDM2 / CDC2 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]

Protocol (from reference)

Solubility (25°C)

In vitro

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.


Chemical Information

Molecular Weight 368.29


CAS No. 13739-02-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C2=O)C=C(C=C3OC(=O)C)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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