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.

PKM2/PDK1-IN-1 is a dual inhibitor targeting pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase kinase 1 (PDK1). It demonstrates significant biological activity by inhibiting the proliferation of non-small cell lung cancer (NSCLC) cells and inducing apoptosis. This compound promotes intercellular reactive oxygen species (ROS) production and modulates apoptotic proteins, engaging both mitochondrial and death receptor pathways in cancer cell death. Its unique mechanism makes it a valuable tool for research in cancer biology and therapeutic development.

PDK1/Akt/Flt dual pathway inhibitor selectively targets the PDK1/Akt/Flt signaling pathways, crucial for cell survival and proliferation. This compound demonstrates significant inhibitory activity, making it a valuable tool for research in cancer biology and therapeutic development. It can be utilized to explore the roles of these pathways in oncogenesis and to assess potential therapeutic strategies against malignancies driven by aberrant PDK1/Akt/Flt signaling.

PDK1-IN-1 is a selective inhibitor of PDK1, which plays a crucial role in cellular signaling pathways related to growth and survival. Additionally, it exhibits inhibitory effects on other kinases, including FGFR3, NTRK3, RP-S6K, and WEE1, as well as microtubule affinity regulating kinase (MARK). This compound is valuable for research applications in the study of myeloproliferative disorders, cancer, and neurodegenerative diseases such as Alzheimer's disease.

Sexangularetin 3-sophoroside is an activator of PDK1 and Akt phosphorylation pathways, demonstrating significant neuroprotective effects. This compound restores levels of phosphorylated GSK-3β protein and functions as a reactive oxygen species (ROS) inhibitor. Additionally, it modulates the expression of superoxide dismutase 1 and catalase mRNA, making it a valuable tool for research related to neurodegenerative conditions such as Parkinson’s disease.