pdk-1

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

MP7 (PDK1 inhibitor) is an inhibitor of phosphoinositide-dependent kinase-1 (PDK1).

PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.

PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1 without affecting other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and activation of S6K.

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.

GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.

BX517 (PDK1 inhibitor 2) is a potent and selective inhibitor of PDK1.

RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.

6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma, adenocarcinoma, multiple myeloma, psoriasis, prostate cancer, and Alzheimer's disease.

PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

PS10 is a broad-spectrum PDK inhibitor that inhibits PDK2, PDK4, PDK1, and PDK3. It significantly increases pyruvate dehydrogenase complex activity, and is used in research on obesity and type 2 diabetes.

PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).

Osu03012 (AR-12) is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity.

PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).

Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.

PDK1-IN-3 (Compound C) is a PDK1 inhibitor with an IC50 value of 34 nM.

PDK1-IN-4 (Compound R-29) is an inhibitor of PDK1, applicable for lung cancer research.

PDK1-IN-5 is a selective inhibitor of PDK1 that reduces phosphorylation levels to activate PDH. This compound effectively reverses the Warburg effect by increasing acetyl-CoA, reducing lactate, elevating mitochondrial ROS, and subsequently inducing apoptosis, shifting cellular energy metabolism from glycolysis to oxidative phosphorylation. PDK1-IN-5 strongly inhibits tumor growth in vivo without causing systemic toxicity and can be used in research on lung adenocarcinoma, human non-small cell lung adenocarcinoma, gastric cancer, and colorectal cancer.

PKM2/PDK1-IN-1, a shikonin thioether derivative, serves as a dual inhibitor for PKM2/PDK1. This compound effectively inhibits the proliferation and induces apoptosis in NSCLC cells. It promotes intercellular ROS production and modulates apoptotic proteins, engaging in both mitochondrial and death receptor pathways [1].

NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1/cyclinB, CDK2/cyclinA3, CDK1/CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

(R)-PS210, the R enantiomer of PS210, is a substrate-selective allosteric PDK1 activator with an (AC50 of 1.8 μM).