For research use only.

Catalog No.S1721

2 publications

Azathioprine Chemical Structure

Molecular Weight(MW): 277.26

Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

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10mM (1mL in DMSO) USD 130 In stock
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Biological Activity

Description Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
Rac1 [1]
In vitro

Azathioprine suppresses the activation of Rac1 target genes such as mitogen-activated protein kinase kinase (MEK), NF-kappaB, and bcl-x(L), leading to a mitochondrial pathway of apoptosis in primary human CD4+ T lymphocytes. Azathioprine thus converts a costimulatory signal into an apoptotic signal by modulating Rac1 activity. [1] Azathioprine-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. [2] Azathioprine (1 mM) restores ATP levels and arrests cell injury, while culture in glucose-enriched media augments ATP levels and ameliorates cell death. Azathioprine reduces viability 5-34% at day 1 and 42-92% by day 4. [3] Azathioprine decreases the viability of hepatocytes and induces the following events in primary culture of isolated rat hepatocytes: intracellular reduces glutathione (GSH) depletion, metabolic activity reduction, and lactate dehydrogenase release. Azathioprine effect on hepatocytes is associated with swelling and increased oxygen consumption of intact isolated rat liver mitochondria. [4]

In vivo Azathioprine combined with cyclosporin A and prednisolone has resulted in survival of 14 out of 15 grafts (93%), compared with 11 out of 14 (79%) in the group treated with cyclosporin A alone in mouse-rat brain xenograft. [5]


Solubility (25°C)

In vitro DMSO 54 mg/mL (194.76 mM)
Water Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 277.26


CAS No. 446-86-6
Storage powder
in solvent
Synonyms N/A
Smiles C[N]1C=NC(=C1SC2=C3[NH]C=NC3=NC=N2)[N+]([O-])=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04109300 Not yet recruiting Genetic: HLADQA1*05A>G screening|Other: Standard of Care Inflammatory Bowel Diseases|Ulcerative Colitis|Crohn Disease Western University Canada September 1 2020 Not Applicable
NCT03350633 Completed Drug: Tocilizumab Injection|Drug: Azathioprine Neuromyelitis Optica Spectrum Disorders|Neuromyelitis Optica Tianjin Medical University General Hospital November 1 2017 Phase 2|Phase 3
NCT02598596 Recruiting Biological: Pegloticase|Drug: Azathioprine Gout Ampel BioSolutions LLC|IND 2 Results LLC December 2015 Phase 2
NCT01160276 Completed Drug: cyclosporine+colchicine|Drug: tacrolimus Renal Replacement Therapies Assistance Publique - Hôpitaux de Paris|Institut National de la Santé Et de la Recherche Médicale France May 2010 Phase 1
NCT00987116 Completed Drug: Prednisone - Azathioprine Myasthenia Gravis Assistance Publique - Hôpitaux de Paris June 2009 Phase 4

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID