Ruxolitinib
JAK inhibitor / Potent and selective JAK1&2 inhibitor, IC50s=2.7, 4.5 and 322 nM forJAK1, JAK2 and JAK3 respectively.1 Blocks IL-6 signaling (IC50=281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50=127 nM).2 Inhibits the proinflammatory secretome of senescent cells.3 The JAK1 S646P mutant is highly sensitive to ruxolitinib.4 Clinically useful cancer chemotherapeutic.
Biochemicals & reagents
941678-49-5
INCB 018424
1) Verstovsek et al. (2009), Therapeutic potential of JAK2 inhibitors; Hematology Am. Soc. Hematol. Educ. Program, 2009(1) 636 2) Quintas-Cardama et al. (2010), Preclinical characterization of the selective JAK1/2 inhibitor INCB01824: Therapeutic implications for the treatment of myeloproliferative neoplasms; Blood, 115 3109 3) Farr et al. (2017) Targeting cellular senescence prevents age-related bone loss in mice; Nat. Med., 23 1072 4) Li et al. (2017) Identification of a novel functional JAK1 S646P mutation in acute lymphoblastic leukemia; Oncotarget, 8 34687
-20°C
TARGET: Kinase -- PATHWAY: Cytokine; Proliferation; JAK/STAT; Cholesterol metabolism -- DISEASE AREA: Inflammation; CancerAtherosclerosis