Description

Product Description

Ruxolitinib Phosphate is a synthetic small-molecule compound belonging to the class of Janus kinase inhibitors (JAK inhibitors). It specifically targets JAK1 and JAK2—key enzymes responsible for transducing signals from cytokine receptors to the nucleus through the JAK-STAT (Signal Transducer and Activator of Transcription) pathway.

By inhibiting these kinases, Ruxolitinib Phosphate disrupts phosphorylation of STAT proteins, preventing their nuclear translocation and downstream transcriptional activation. This mechanism has made Ruxolitinib an indispensable molecular probe in inflammation research, cytokine biology, and cancer signal transduction studies.

In scientific studies, Ruxolitinib is particularly valuable for dissecting mechanisms of myeloproliferative neoplasms (MPN), autoimmune diseases, and immune cytokine cascades. It provides a clear model for how kinase inhibition affects hematopoiesis, cell proliferation, and immune cell differentiation.

The phosphate form of Ruxolitinib is water-soluble, improving its handling and stability for both in vitro and in vivo research applications. It is extensively used by cell biologists and pharmacologists for investigating the molecular consequences of JAK inhibition.

Biological Context and Importance

The JAK-STAT pathway is a fundamental signaling cascade that transmits extracellular cytokine stimuli to the nucleus, leading to the transcription of genes involved in immunity, proliferation, and apoptosis. Dysregulation of this pathway contributes to inflammatory disorders, cancers, and autoimmune diseases.

Ruxolitinib Phosphate inhibits both JAK1 and JAK2 with nanomolar potency (IC₅₀ ≈ 3.3 nM for JAK1 and 2.8 nM for JAK2). This high specificity enables researchers to analyze cytokine-dependent signaling with minimal off-target interference.

In immunology research, Ruxolitinib has been shown to modulate pathways driven by interleukins (IL-2, IL-6, IL-12, IL-23) and interferons (IFN-α, IFN-γ), providing a model for anti-inflammatory and immunomodulatory investigations.

In oncology research, it offers insight into how JAK-STAT hyperactivation contributes to tumor growth, survival, and immune evasion.

Research Applications

• Signal Transduction Studies: Inhibition of JAK-STAT phosphorylation and downstream gene expression.

• Inflammation and Cytokine Research: Evaluation of cytokine suppression, particularly IL-6, IFN-γ, and IL-23.

• Cancer Biology: Used to model JAK2-dependent tumorigenesis, especially in leukemia and lymphoma cell lines.

• Autoimmune Mechanism Studies: Modulation of Th1/Th17 pathways in autoimmune conditions.

• Hematopoietic Regulation: Understanding erythropoietin and thrombopoietin signaling.

Product Specifications

Mechanism of Action

Ruxolitinib Phosphate competitively inhibits the ATP-binding site of Janus kinases JAK1 and JAK2. These kinases are integral to cytokine receptor signaling, where receptor engagement activates JAKs, leading to phosphorylation of STAT transcription factors.

Key Mechanistic Steps:

1. Inhibition of JAK Autophosphorylation:
   Prevents receptor-associated kinases from phosphorylating themselves and downstream targets.

2. Blockade of STAT Activation:
   Prevents STAT1, STAT3, and STAT5 from translocating to the nucleus and initiating transcription.

3. Suppression of Cytokine Signaling:
   Reduces transcription of cytokine-responsive genes related to inflammation and survival.

4. Modulation of Immune Function:
   Downregulates inflammatory cytokines and immune effector gene expression, providing a model for immunoregulation.

Molecular Pathways Affected:

• JAK-STAT Pathway

• NF-κB Modulation

• IL-6 and IFN Signaling Suppression

• Apoptotic Pathways via STAT3 Inhibition

  

Side Effects

In cell culture and in vivo models, Ruxolitinib Phosphate may exhibit concentration-dependent cytotoxicity due to suppression of key cytokine pathways. Observed laboratory effects include:

• Reduction in hematopoietic cell proliferation.

• Inhibition of interferon-mediated signaling.

• Potential induction of apoptosis in cytokine-dependent cells.

• Modulation of oxidative stress markers.

Researchers are advised to handle the compound with appropriate protective measures and use in controlled laboratory settings only.

Keywords

Ruxolitinib Phosphate, CAS 1092939-17-7, JAK1/2 inhibitor, cytokine signaling, inflammation research, STAT phosphorylation, immune modulation, hematopoietic studies, kinase inhibitor, oncology reagent, high purity compound.

Shipping Guarantee

All Ruxolitinib Phosphate shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We Ruxolitinib Phosphate ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

Payment Support

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Disclaimer

All Ruxolitinib Phosphate products are intended for laboratory research use only. They are not suitable for human or veterinary use, diagnosis, or treatment. The information provided is for scientific reference purposes only. Researchers must handle materials following institutional biosafety and chemical safety guidelines.