Home Cell Cycle Rho inhibitor Azathioprine For research use only.

Azathioprine

Synonyms: BW 57-322

Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

Azathioprine Chemical Structure

Azathioprine Chemical Structure

CAS No. 446-86-6

Purity & Quality Control

Azathioprine Related Products

Signaling Pathway

Rho Signaling Pathways

Rho Signaling Pathway

Biological Activity

Description Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
Targets
Rac1 [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06066957 Recruiting
Cytomegalovirus Infections|Transplant-Related Disorder
University of Pennsylvania|Merck Sharp & Dohme LLC
 April 4 2024 Phase 2
NCT05859191 Recruiting
Systemic Lupus Erythematosus|Physiopathology
University Hospital Tours|Research Center for Respiratory Diseases Inserm U1100
 July 21 2023 --
NCT05994716 Enrolling by invitation
Inflammatory Bowel Diseases|Crohn Disease|Ulcerative Colitis
Research and Practical Clinical Center for Diagnostics and Telemedicine Technologies of the Moscow Health Care Department|Sechenov University
 April 25 2023 Not Applicable
NCT05349006 Not yet recruiting
Central Nervous System Inflammation|MOG-IgG Associated Disease
Hospices Civils de Lyon
 January 1 2023 Phase 3
NCT05370690 Unknown status
Uveitis
University Hospital Brest
 May 1 2022 --
NCT05321485 Unknown status
Inflammatory Bowel Diseases|Crohn Disease|Ulcerative Colitis
Maxima Medical Center
 March 16 2022 Not Applicable

Chemical Information & Solubility

Molecular Weight 277.26 Formula

C9H7N7O2S
CAS No. 446-86-6 SDF Download Azathioprine SDF
Smiles CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (194.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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