CP-690550

JAK3 Inhibitor

CP-690550 (Tofacitinib) specifically inhibits JAK3, which has a pivotal role in cytokine signal transduction that governs lymphocyte survival, proliferation, differentiation, and apoptosis [1].
In experimental models, treatment with CP-690550 decreases IL-6 production, a critical cytokine that drives inflammation [2]. Moreover, it has been shown that CP-690550 also inhibits TNF-induced chemokine expression [3].

References:

1. Wu W. & Sun X., 2012. Janus kinase 3: the controller and the controlled. Acta Biochim Biophys Sin. 44(3):187-96.
2. Milici A. et al., 2008. Cartilage preservation by inhibition of Janus kinase 3 in two rodent models of rheumatoid arthritis. Arthritis Res Ther. 10: R14.
3. Sanna Rosengren S. et al., 2012. The JAK inhibitor CP-690,550 (tofacitinib) inhibits TNF-induced chemokine expression in fibroblast-like synoviocytes: autocrine role of type I IFN. Ann Rheum Dis 71:440-7.

Figures

Effect of CP-690550 on HEK-Blue™ IFN-α/β cell response to type I and type III IFNs: HEK‑Blue™ IFN-α/β cells were incubated with 3 U/ml hIFN-α2b (grey), 1 U/ml hIFN-β1 (purple) or 10 ng/ml hIL-29 (hIFN-λ1) (red) and increasing concentrations of CP‑690550. After 24h incubation, IFN-induced ISG activation was assessed by measuring SEAP levels in the supernatant using QUANTI‑Blue™. Percentages of maximal response (no inhibitor) for each cytokine are shown.

Specifications

Synonym: Tofacitinib

CAS number: 477600-75-2

Formula: C₁₆H₂₀N₆O

Molecular weight: 312.37

Solubility: 100 mg/ml in DMSO

Purity: ≥96% (HPLC)

Working concentration: 50 nM - 1 µM

Quality control: The absence of bacterial contamination (e.g. lipoproteins and endotoxins) is confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.

Contents

CP-690550 is provided as a solid.

• 5 mg CP-690550

CP-690550 is shipped at room temperature.

Store at -20°C.

Solid product is stable for 2 years when properly stored.