research use only

Azathioprine Rho inhibitor

Cat.No.S1721

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.
Jump to

Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (194.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 277.26 Formula

C9H7N7O2S

Storage (From the date of receipt)
CAS No. 446-86-6 Download SDF Storage of Stock Solutions

Synonyms BW 57-322 SMILES CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-]

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Rac1
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. This compound thus converts a costimulatory signal into an apoptotic signal by modulating Rac1 activity. This compound-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. This chemical (1 mM) restores ATP levels and arrests cell injury, while culture in glucose-enriched media augments ATP levels and ameliorates cell death. It reduces viability 5-34% at day 1 and 42-92% by day 4. This agent 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. Its effect on hepatocytes is associated with swelling and increased oxygen consumption of intact isolated rat liver mitochondria.

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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15226385/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8566182/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-23)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07616154 RECRUITING
Sickle Cell Disease
St. Jude Children's Research Hospital
2026-09 PHASE2
NCT07352566 NOT_YET_RECRUITING
Psoriasis; Atopic Dermatitis
University of California, San Francisco
2026-08-01 PHASE4
NCT05584228 NOT_YET_RECRUITING
Crohn Disease
Nantes University Hospital
2026-10-01
NCT07659353 NOT_YET_RECRUITING
Chrohn's Disease
University Hospital Schleswig-Holstein
2026-08-01 PHASE4
NCT02939573 RECRUITING
Primary Cutaneous Vasculitis; Cutaneous Polyarteritis Nodosa; IgA Vasculitis; Henoch-Schönlein Purpura
University of Pennsylvania
2017-01-01 PHASE2
NCT07619898 NOT_YET_RECRUITING
Colitis; Hepatitis; Melanoma (Skin Cancer)
Therakos LLC
2026-07 PHASE2

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map