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Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block...

Nitric oxide synthase (NOS) catalyzes the conversion of L-arginine to nitric oxide (NO) and citrulline. Methyl-L-NIO (hydrochloride) is a competitive nitric oxide synthase (NOS) inhibitor that competes with L-arginine for the amino acid binding site. It is a more potent inhibitor of nNOS (Ki = 3.0 µM) than eNOS (Ki...

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative compounds which act as protein tryrosine kinase blockers. PTK inhibitors which preferentially inhibit the epidermal growth...

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Olomoucine is a cdk inhibitor that acts by competing for the ATP binding site of the kinase. This purine derivative is an inhibitor for CDC2/cyclin B (IC50 = 7 µM), Cdk2/cyclin A (IC50...

The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for...

The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4. Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the...

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block...

Apigenin is a flavonoid compound found in many fruits and vegetables that selectively inhibits casein kinase 2 (CK2). Apigenin inhibits CK2 activity in the renal cortex with an IC50 value of 30 µM to improve renal function in a rat model of glomerulonephritis. CK2 inhibition by 20 µM apigenin decreases the...