HTH-01-015 is a potent and selective inhibitor of NUAK1 kinase, a member of the AMPK family that are that are activated by the LKB1 (liver kinaseB1) tumour suppressor kinase and involved in development and proliferation.
HTH-01-015 is a potent and selective inhibitor of NUAK1 kinase, a member of the AMPK family that are that are activated by the LKB1 (liver kinaseB1) tumour suppressor kinase and involved in development and proliferation. HTH-01-015 has an IC50 of 100 nM for NUAK1, >100-fold higher than NUAK2, and has no significant inhibition of 139 other kinases tested, including ten AMPK-related kinase family members. Treatment with HTH-01-015 was found to suppress proliferation, restricting cells from entering into mitosis.
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