SERP
Comments:
AZ 960 is a moderately selective, ATP competitive JAK2 inhibitor with IC50 of <3 nM and a 3-fold selectivity over JAK3. It has been tested in a panel of 83 protein kinases at three inhibitor concentrations (0.01, 0.10, and 1.0 uM). AZ960 inhibited 11 kinases greater than 50% at a concentration of 0.1 uM. No reports of any additional off target profiling has been found. AZ960 is extensively profiled in various cellular assays at various levels with temporal control:
o In a “close to target assay”, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average IC50 of 15 nM and exhibits 15-30 -fold sensitivity for TEL-JAK2-driven STAT5 phosphorylation compared with cell lines driven by other JAK kinase family members.
o In a “proximal response assay” (after gene regulation), AZ960 inhibits BCL-XL gene expression as well as Pim1 and Pim2 expression (known to be regulated by BCL-XL) in SET-2 Cells.
o In a “phenotypic assay”, AZ960 dose dependently inhibited SET-2 cell proliferation (after inhibition of STAT3/5 phosphorylation).
AZ960 has not been reported to be used in any model organisms. However, several other JAK2 inhibitors are available with various selectivity profiles of which several have reported in vivo data (even clinical data).
Many JAK2 inhibitors with various potency and selectivity profiles exists of which many have been used as pharmacological in vivo tools. There is to my knowledge no public information about the use of AZ-960 in any model organisms. Several of JAK2 inhibitors are in the chemical probes portal.
(last updated:
12 Oct 2021 )