pdhk2

AZD7545 is a potent PDHK inhibitor.

PDHK1-IN-3 (Compound 29) is a selective inhibitor of PDHK1, demonstrating an IC50 of 0.028 μM for PDHK1 and an IC50 of 0.120 μM for PDHK2. It inhibits PDHK1 activity by forming a covalent bond with Lys299 in the enzyme. PDHK1-IN-3 is applicable to research on autoimmune diseases, inflammatory conditions, and cancer.

PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinase 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and 0.015 μM for PDHK2. PDHK1-IN-2 has the potential to regulate immune cell metabolism and correct mitochondrial dysfunction, making it a promising candidate for research in autoimmune diseases, inflammatory conditions, and cancer.

PDHK-IN-3 (compound 7) is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK) with IC50 values of 0.21 μM for PDHK2 and 1.54 μM for PDHK4 [1].

PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK, targeting PDHK2 (IC50: 0.0051 μM) and PDHK4 (IC50: 0.0122 μM), with potential applications in cancer research.

TM-1 is a potent pyruvate dehydrogenase kinase (PDHK) inhibitor that inhibits the activity of PDHK1 (IC50: 2.97 μM) and PDHK2 (IC50: 5.2 μM). TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation and inhibits cancer cell proliferation.

PDHK-IN-5 is a potent inhibitor of PDHK, acting on PDHK2 (IC50: 0.006 μM) and PDHK4 (IC50: 0.0329 μM), which are drug targets for many diseases including diabetes and cancer. PDHK-IN-5 has the potential to be investigated in cancer diseases.