AZ960,905586-69-8

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AZ960

CAS No. : 905586-69-8

MCE 国际站：AZ960

产品活性：AZ960是高效选择性的JAK2激酶抑制剂，K_i值为0.45 nM。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis  |  Anti-infection

作用靶点：JAK  |  Apoptosis  |  Parasite  |  Virus Protease

In Vitro: AZ960 inhibits Jak2 kinase with a K_i of 0.45 nM. Z960 possesses much less potent activity against Jak1, 3, and TYK2. AZ960 is active against other kinases, including TrkA, Aurora-A, and FAK, with IC₅₀ of around 0.1 μM. AZ960 effectively induces 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.
AZ960 potently inhibits the clonogenic growth and induces apoptosis of freshly isolated acute myelogenous leukemia cells from patients in association with cleavage of caspase 3 and down regulation of anti-apoptotic Bcl-xL proteins.
AZ960 has a K_i of 1.25 μM for T. brucei extracellular signal-regulated kinase 8 (TbERK8). It inhibits TbERK8 with an IC₅₀ of 120 nM.

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