PDK1

OSU-03012 is a novel celecoxib derivative, without cyclooxygenase-2 inhibitory activity, capable of inducing apoptosis in various cancer cells types.

PHT-427 is a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.

BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis.

BX-912 is an inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1).

NVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM).

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.

GSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM).

BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM).

PS 48 is an allosteric phosphoinositide-dependent protein kinase-1 (PDK1) activator (Kd = 10.3 μM).

PDK1 inhibitor, potent, ATP-competitive and selective dual PI3K and PDPK1 inhibitor (IC50 values 34 nM and 94 nM for PDK1 and p-T308-PKB inhibition, respectively.

KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.

PS210 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively.