PDK-1
3-Phosphoinositide-dependent protein kinase 1
PDK-1 (3-Phosphoinositide-dependent protein kinase 1), a member of the protein A, G and C (AGC) family of proteins, is a Ser/Thr protein kinase. PDK-1, is the pivotal node in the PI3K pathway, has a key role in insulin and growth-factor signalling through phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B.
PDK-1 is responsible for the regulation of cell proliferation and migration and it also has been found to play a key role in different cancers, pancreatic and breast cancer amongst others. Many cancer-driving mutations induce activation of PDK-1 targets including Akt, S6K (p70 ribosomal S6 kinase) and SGK. Thus, PDK1 is a critical activator of multiple pro-survival and oncogenic protein kinases, for which it has garnered considerable interest as an oncology drug target.
All Product Categories
-
PDK-1 Related Products (51)
Related Products (51)
-
Antibodies (2)
-
PDK1-IN-5
0 ImagesCat. No.: HY-179501PDK1-IN-5 is a selective PDK1 inhibitor. PDK1-IN-5 activaties PDH by diminishing phosphorylation level via PDK1 inhibition. PDK1-IN-5 effectively reverses the Warburg effect and shifts cellular energy metabolism from glycolysis toward oxidative phosphorylation by increased acetyl-CoA, reduced lactate, elevated mitochondrial ROS, and subsequent induction of apoptosis. PDK1-IN-5 robustly inhibits tumor growth in vivo without inducing systemic toxicity. PDK1-IN-5 can be used for lung adenocarcinoma, human non-small cell lung adenocarcinoma and gastric colorectal.
-
MG-Lin1
0 ImagesCat. No.: HY-177731MG-Lin1 is a Lin28/Lin28A molecular glue degrader with a DC50 of approximately 0.7 μM. It induces Lin28 degradation via the ubiquitin-proteasome pathway by forming a ternary complex, thereby upregulating the levels of let-7 miRNA and reducing the expression of its downstream oncogenic targets KRAS and PDK1, and inhibiting cancer cell migration. MG-Lin1 can be used in studies of ovarian cancer and choriocarcinoma.
-
CRTh2 antagonist 3
0 ImagesCat. No.: HY-135773CAS No.: 312928-72-6CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.
-
X-370
0 ImagesCat. No.: HY-12482CAS No.: 1280725-80-5X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
-
LDHA/PDKs-IN-2
0 ImagesCat. No.: HY-146978CAS No.: 2490699-44-8LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC50 of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases.
-
PKM2/PDK1-IN-1
0 ImagesCat. No.: HY-149275CAS No.: 3041957-90-5PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.
-
BX-912 (Standard)
0 ImagesCat. No.: HY-11005RCAS No.: 702674-56-4BX-912 (Standard) is the analytical standard of BX-912 (HY-11005). This product is intended for research and analytical applications. BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
-
OSU-03012 (Standard)
0 ImagesCat. No.: HY-10547RCAS No.: 742112-33-0Synonyms: AR-12 (Standard); PDK1 inhibitor AR-12 (Standard)
-
PF-5177624
0 ImagesCat. No.: HY-117885CAS No.: 1350821-45-2PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells.
-
mIDH1-IN-2
0 ImagesCat. No.: HY-175770mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma.
-
BX795 (Standard)
0 ImagesBX795 (Standard) is the analytical standard of BX795 (HY-10514). This product is intended for research and analytical applications. BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
