nuak1

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.

XMD-17-51 has DCLK1 kinase inhibitory activity, inhibits DCLK1 and cell proliferation, and can be used in lung cancer research.

MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).

WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.

XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.

LRRK2/NUAK1/TYK2-IN-1 (compound 226) exhibits inhibitory activity against LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1, demonstrating IC50 values below 10 nM. This compound is useful for research into autoimmune diseases.

NUAK1-IN-1 (Compound 9) is an inhibitor of NUAK1 with an IC50 of 5.012 nM, as well as a CDK4 inhibitor. It is suitable for research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.

NUAK1-IN-2 (Compound 24) is an inhibitor of NUAK1 with an IC50 of 3.162 nM, as well as an inhibitor of CDK2/4/6. It is applicable in research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.

ARUK2010489 (Compound 23) is a potent, selective, and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7, also exhibiting partial inhibitory activity against CDK2, CDK4, and CDK6 at micromolar concentrations, and it is applied in neurological disease research, including mechanistic studies related to Alzheimer’s disease.

ARUK2010694 (Compound 20) is a potent and selective inhibitor of NUAK1, with a pIC50 value of 8.7. It also inhibits the activity of CDK2, CDK4, and CDK6, with inhibition rates of 13%, 63%, and 32% respectively at a concentration of 1 μM. ARUK2010694 is applicable in research on neurological disorders, including Alzheimer's disease (AD).

CCT245737 is an orally active, selective Chk1 inhibitor with an IC50 of 1.3 nM, and is >1,000-fold selective over CHK2 and CDK1.

Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).

UCB9386 is a brain-penetrant and selective inhibitor of Nuak1, with a pIC50 of 10.1. It also inhibits Nuak2 and Kak2, showing approximately 50% inhibition at 10 nM.