Cat. No.: HY-N0283

Diacerein

(Synonyms: Diacerhein; Diacetylrhein)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research.

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

Purity: 98.64%
CAS No.: 13739-02-1
Formula: C₁₉H₁₂O₈
Molecular Weight:368.29

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Diacerein Chemical Structure

CAS No.: 13739-02-1

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

IL-1β

L-type calcium channel

All Interleukin Related Isoforms :

All Calcium Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	CC₅₀	108.2 μM Compound: Diacerein	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 34491054]
RAW264.7	IC₅₀	106.9 μM Compound: Diacerein	Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis	[PMID: 34491054]
RAW264.7	IC₅₀	126.77 μM Compound: Diacerein	Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis	[PMID: 34491054]
RAW264.7	IC₅₀	65.41 μM Compound: Diacerein	Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis	[PMID: 34491054]

In Vitro

Diacerein (Diacerhein; 30-300 μM; 24, 48 h) reduces cell proliferation and viability of chondrosarcoma cells^[1].
Diacerine (30-300 μM; 48 h) causes a SW-1353 cell cycle G2/M arrest^[1].
Diacerein (30-300 μM; 48 h) decreases cyclin B1, CDK1, and CDK2 levels in SW-1353 cell^[1].
Diacerein can relax the agonist-precontracted mouse airway smooth muscle via intracellular and extracellular calcium mobilization which is mediated by switched voltage-dependent L-type Ca²⁺ channels, non-selective cation channels, large-conductance Ca²⁺-activated K⁺ channel, and Na⁺/Ca²⁺ exchangers^[2].

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

Cell Viability Assay^[1]

Cell Line:

Cal-78 and SW-1353 cells
Concentration:

30, 100, and 300 μM
Incubation Time:

24, 48 h
Result:

Inhibited cell growth in a concentration dependent manner in both cell lines.

Cell Cycle Analysis^[1]

Cell Line:

Cal-78 and SW-1353 cells
Concentration:

30, 100, and 300 μM
Incubation Time:

48 h
Result:

Caused a pronounced decrease in the number of cells in the G1 phase, accompanied by a significant increase of the number of S and G2/M phase cells, indicating a G2/M arrest in SW-1353 cells.

Western Blot Analysis^[1]

Cell Line:

Cal-78 and SW-1353 cells
Concentration:

30, 100, and 300 μM
Incubation Time:

24 h
Result:

Induced a small, but not significant change, for the expression of CDK1, whereas the cyclin B1 and CDK2 levels were significantly down-regulated in the case of Cal-78 cells.

In Vivo

Diacerein (Diacerhein; 50, 100, 200 mg/kg; Gavaged; daily; a week) can effectively reduce airway hypertension and improve airway remodeling in asthmatic mice with Ovalbumin (OVA; 3 mg/ml; 200 μl; IP; dissolved with 25 mg/ml Al(OH)3 at day 1, day 8)^[2].
Diacerein (2, 20, 60 mg/kg; daily; oral; at 2 weeks of age transgenic mice; for 5 weeks) reveales a significant reduction not only in cartilage destruction but also in the extent of synovitis and bone erosion in the Tg197 transgenic murine model of RA^[3].

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

Animal Model:

Male BALB/c mice at 6-8 weeks of age^[2]
Dosage:

50, 100, 200 mg/kg
Administration:

Gavaged; daily; a week
Result:

Reduced systematic inflammation and mucus secretion in vivo.
Exhibited anti-inflammatory property to significantly reduce inflammation and repair damaged airway.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 13739-02-1
Appearance Solid
Molecular Weight 368.29
Formula C₁₉H₁₂O₈
Color Light yellow to yellow
SMILES

O=C(C(C=C1C2=O)=CC(OC(C)=O)=C1C(C3=C2C=CC=C3OC(C)=O)=O)O
Synonyms

Diacerhein; Diacetylrhein
Structure Classification
- Quinones
- Anthraquinones
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (7)

All

Sort by:

Journal Impact Factor

Br J Cancer

PARP inhibition leads to synthetic lethality with key splicing-factor mutations in myelodysplastic syndromes. [Abstract]

2024 Jul;131(2):231-242. PMID: 38806724
Cell Rep

Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]

2025 May 14;44(5):115712. PMID: 40372911
Ecotoxicol Environ Saf

Factors ameliorate pro-inflammatory microglia polarization through inhibition of reactive astrocytes induced by 2-chloroethanol. [Abstract]

2023 Aug:261:115130. PMID: 37311391
Biochem Pharmacol

Diacerein protects against Ovariectomy-Induced bone loss via reversal of NRF2 epigenetic suppression. [Abstract]

2026 Jan 24:247:117748. PMID: 41587594
Biochem Pharmacol

FTO aggravates podocyte injury and diabetic nephropathy progression via m6A-dependent stabilization of ACC1 mRNA and promoting fatty acid metabolism. [Abstract]

2025 May:235:116819. PMID: 39988261
Molecules

Rapid Discovery of CD38 Inhibitor via DNA-Encoded Natural Product Library Screening. [Abstract]

2026 Mar 5;31(5):864. PMID: 41828851
J Inflamm Res

Interleukin 1β Mediates the Pathogenesis of Nasal Mucosal Epithelial Barrier Dysfunction in Allergic Rhinitis. [Abstract]

2024 Nov 19:17:9071-9085. PMID: 39588138

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (33.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7153 mL

13.5763 mL

27.1525 mL

5 mM

0.5431 mL

2.7153 mL

5.4305 mL

10 mM

0.2715 mL

1.3576 mL

2.7153 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 1% CMC/saline water

Solubility: 5 mg/mL (13.58 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Birgit Lohberger, et al. Diacerein retards cell growth of chondrosarcoma cells at the G2/M cell cycle checkpoint via cyclin B1/CDK1 and CDK2 downregulation. BMC Cancer. 2015 Nov 10:15:891. [Content Brief]

[2]. Shi S, Xue L, Han S, et al. Anti-Contractile and Anti-Inflammatory Effects of Diacerein on Isolated Mouse Airways Smooth Muscle and Mouse Asthma Model. Front Pharmacol. 2020;11:560361. [Content Brief]

[3]. Eleni Douni, et al. Attenuation of inflammatory polyarthritis in TNF transgenic mice by diacerein: comparative analysis with dexamethasone, methotrexate and anti-TNF protocols. Arthritis Res Ther. 2004;6(1):R65-R72. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7153 mL	13.5763 mL	27.1525 mL	67.8813 mL
	5 mM	0.5431 mL	2.7153 mL	5.4305 mL	13.5763 mL
	10 mM	0.2715 mL	1.3576 mL	2.7153 mL	6.7881 mL
	15 mM	0.1810 mL	0.9051 mL	1.8102 mL	4.5254 mL
	20 mM	0.1358 mL	0.6788 mL	1.3576 mL	3.3941 mL
	25 mM	0.1086 mL	0.5431 mL	1.0861 mL	2.7153 mL
	30 mM	0.0905 mL	0.4525 mL	0.9051 mL	2.2627 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Diacerein

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Natural Product Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Lipid Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Medicine Food Homology Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Traditional Chinese Medicine Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Angiogenesis-Related Compound Library

Rare Diseases Drug Library

Antidepressant Compound Library

Protein-protein Interaction Inhibitor Library

Anti-inflammatory Traditional Chinese Medicine Active Compound Library

Plant-Sourced Natural Product Library

Human Metabolite Library

Non-steroidal Anti-Inflammatory Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

FDA-Approved Traditional Chinese Medicine Active Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Radioprotector Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Natural Product and Natural Product-Like Compound Library

Heat-Clearing and Detoxification Traditional Chinese Medicine Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Ancient Chinese Classical Formulas Traditional Chinese Medicine Active Compound Library

Mass Spectrometry Human Metabolite Library

Diarrhea-Related Traditional Chinese Medicine Active Compound Library

Mongolian Medicine Compound Library

Quinones Library

RNA Binding Bioactive Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Diacerein

All Interleukin Related Isoforms

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Diacerein Related Classifications

HY-N0283 Related Classifications