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United States (Change Country)AZ 960 Chemical Structure
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 μM. AZ960, a novel inhibitor of Jak2 kinase, effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1–infected 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. [1][2]
[] THE JOURNAL OF BIOLOGICAL CHEMISTRY November 21, 2008;283:32334–32343
[] Mol Cancer Ther 2010;9:3386-3395
| Molecular Weight (WM): | 354.36 |
|---|---|
| Formula: | C18H16F2N6 |
| Solubility(R.T.:25°C): | DMSO 71mg/mL |
| Water <1mg/mL | |
| Ethanol 3mg/mL |
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;Claude HAAN Université du Luxembourg AZ 960 purchased from Selleck
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