AZA1 is a Potent Dual Inhibitor of Rac1 and Cdc42

Prostate cancer is the leading cause of cancer and the second leading cause of cancer-related deaths in men. Rho GTPases such as Rac, Cdc42, and RhoA are signaling proteins. They regulate cytoskeleton organization, cell cycle progression, cell survival, and migration directly contributing to tumor growth and progression. Cdc42 additionally...

CID44216842 is a Potent Cdc42-Selective Guanine Nucleotide Binding Lead Inhibitor

Cdc42, a small GTPase of the Rho family, plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal disorders. Therefore, Cdc42 inhibitors will be useful in probing molecular pathways and could...

ZINC69391 is a Specific Rac1 Inhibitor and Apoptosis Inducer

Rho-GTPases are molecular switches that cycle between an inactive GDP-bound form and an active GTP-bound form. Guanine nucleotide exchange factors (GEFs) catalyze nucleotide exchange and mediate activation in this cycle, While GTPase-activating proteins (GAPs) stimulate GTP hydrolysis and inactivate the GTPase. Only the active GTP-bound state binds to downstream...

THZ-P1-2 is a Selective PI5P4K Inhibitor

Phosphatidylinositol 5-phosphate (PI-5-P) is one of the seven phosphoinositides. They regulate a wide range of cellular functions. They localize in the nucleus, Golgi, endoplasmic reticulum, and at the plasma membrane. PI-5-P is an oxidative stress-induced regulator of AKT activation. The phosphorylation of the low abundance phosphoinositide PI-5-P at the...

TED-347 is an Irreversible and Covalent YAP-TEAD Protein-Protein Interaction Inhibitor

Yap1, also known as Yap, is a protein that acts as a transcription regulator by activating the transcription of genes involved in cell proliferation and inhibiting apoptosis. Specifically, Yap1 is inhibited in the hippopotamus signaling pathway, which can control organ size and inhibit tumors. Besides, hippopotamus signaling regulates Yap1...

PD-089828 is an Inhibitor of FGFR-1, PDGFR-β, EGFR and c-Src Tyrosine Kinase

Protein tyrosine kinases comprise a group of enzymes. They catalyze the phosphorylation of certain proteins on specific tyrosine residues. The growth factor receptor tyrosine kinases are a subfamily. The kinases are activated on the high-affinity binding of growth factors to their cognate receptors. Members of this subfamily include PDGFR...

OT-82 is an Orally Active NAMPT Inhibitor with Antineoplastic Activity

Treatment of hematopoietic (HP) malignancies such as leukemia, lymphoma, and myeloma need improvement due to the drug high toxicity. Some effective anticancer agents are tissue-selective but not cancer-specific targets. These agents cannot distinguish normal and transformed cells. Besides they are usually against lineage-specific metabolic deficiency or lineage-specific surface antigen,...