[HTML][HTML] AMP-activated protein kinase selectively inhibited by the type II inhibitor SBI-0206965
Inhibition of the metabolic regulator AMP-activated protein kinase (AMPK) is increasingly
being investigated for its therapeutic potential in diseases where AMPK hyperactivity results
in poor prognoses, as in established cancers and neurodegeneration. However, AMPK-
inhibitory tool compounds are largely limited to compound C, which has a poor selectivity
profile. Here we identify the pyrimidine derivative SBI-0206965 as a direct AMPK inhibitor.
SBI-0206965 inhibits AMPK with 40-fold greater potency and markedly lower kinase …
being investigated for its therapeutic potential in diseases where AMPK hyperactivity results
in poor prognoses, as in established cancers and neurodegeneration. However, AMPK-
inhibitory tool compounds are largely limited to compound C, which has a poor selectivity
profile. Here we identify the pyrimidine derivative SBI-0206965 as a direct AMPK inhibitor.
SBI-0206965 inhibits AMPK with 40-fold greater potency and markedly lower kinase …