货号 | 14703S |
供应商 | CST |
背景 | Tofacitinib is a cell permeable Janus kinase (JAK) inhibitor with demonstrated preference to inhibiting JAK1 and JAK3 (1). Tofacitinib inhibits JAK isoforms 1, 2, and 3 with IC50 values of 6.1, 12, and 8.0 nM, respectively; the reported IC50 value relative to Tyk2 is 176 nM (2). Research studies show that tofacitinib primarily blocks γc cytokine receptors and inhibits cytokine production, which suggests that tofacitinib blocks cytokine action during both innate and adaptive responses (1,3). The overall effect of tofacitinib is to reduce inflammatory responses through selective inhibition of JAK family members (4). |
存放说明 | -20C |
参考文献 | 1 . Ghoreschi, K. et al. (2011) J Immunol 186, 4234-43. 2 . Haan, C. et al. (2011) Chem Biol 18, 314-23. 3 . Ju, W. et al. (2011) Blood 117, 1938-46. 4 . Changelian, P.S. et al. (2003) Science 302, 875-8. |
Chemical structure of Tofacitinib. | |
Western blot analysis of extracts from NK-92 cells, serum-starved overnight and untreated (-) or treated with Human Interleukin-2 (hIL-2) #8907 (10 ng/ml, 15 min; +), either with or without Tofacitinib pretreatment (1 hr) at the indicated concentrations, using Phospho-Jak3 (Tyr980/981) (D44E3) Rabbit mAb #5031, Jak3 (D1H3) Rabbit mAb #8827, Phospho-Stat3 (Tyr705) (D3A7) XP® Rabbit mAb #9145, Stat3 (79D7) Rabbit mAb #4904, and β-Actin (D6A8) Rabbit mAb #8457. |