AZ 960 is a novel small molecule JAK2 kinase inhibitor with an IC50 and Ki of 3 mM and 0.45 nM in vitro, respectively. AZ960 was also shown to be active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 ¦ÌM. AZ960, a novel inhibitor of Jak2 kinase, effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1¨Cinfected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1. Interestingly, AZ960 increased levels of Bcl-xL in MT-1 and MT-2 cells in association with accumulation of cAMP response element-binding protein bound to the Bcl-xL promoter as measured by chromatin immunoprecipitation assay. Importantly, genetic inhibition of Bcl-xL by a small interfering RNA potentiated antiproliferative effects of AZ960 in MT-1 cells.

June 21, 2017

prudect name : AZ 960 is a novel small molecule JAK2 kinase inhibitor with an IC50 and Ki of 3 mM and 0.45 nM in vitro, respectively. AZ960 was also shown to be active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 ¦ÌM. AZ960, a novel inhibitor of Jak2 kinase, effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1¨Cinfected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1. Interestingly, AZ960 increased levels of Bcl-xL in MT-1 and MT-2 cells in association with accumulation of cAMP response element-binding protein bound to the Bcl-xL promoter as measured by chromatin immunoprecipitation assay. Importantly, genetic inhibition of Bcl-xL by a small interfering RNA potentiated antiproliferative effects of AZ960 in MT-1 cells.
AZ 960

Synonyms: CAS NO: 905586-69-8Molecular Formula: C₁₈H₁₆F₂N₆Molecular Weight: 354.36Purity: 98% minSolubility: In DMSOStorage: −20°C

187389-52-2 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18497599