6RK73 is a Covalent Irreversible and Specific UCHL1 Inhibitor
Approximately 90% of breast cancer-related deaths are due to metastasis. During the metastasis process, epithelial-mesenchymal transition (EMT) plays an important role. The secreted cytokine transforming growth factor-β (TGFβ) can induce it. Breast cancer has multiple subtypes with distinct metastatic potential based on genetic and clinical features. The most aggressive...
ADH-503 is an Orally Active and Allosteric CD11b Agonist
Integrin αMβ2 (CD11b/CD18) is a multifunctional integrin expressed on myeloid cells. In addition, CD11b/CD18 is an integrin molecule and plays an important role in their trafficking and cellular functions in inflamed tissues. Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal malignancy in which very limited responses to immunotherapy have been observed....
CNX-500 is a Covalent Btk Inhibitor (CC-292) Linked to Biotin Chemically
Bruton’s tyrosine kinase (Btk) is a kinase. B cells and myeloid cells expressed exclusively. It plays a vital role in B cells. Btk plays an essential role in the B cell receptor (BCR) signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn...
DS-437 is a Dual PRMT5/7 Inhibitor
Protein arginine methyltransferases are a class of enzymes. They transfer a methyl group from the cofactor S-adenosylmethionine (SAM) onto the arginine omega nitrogens of substrate proteins, including histones. There are three subclasses based on their product specificity: type I, II, and III PRMTs asymmetrically dimethylate, symmetrically dimethylate, and monomethylate their...
BAY-985 is an Orally Active and ATP-Competitive TBK1/IKKε Inhibitor
The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homolog IKKε plays an important role in cellular pathways. And, as we all know, these kinases belong to the nuclear factor κB family. In this article, we will introduce a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε,...
HKI-357 is an Irreversible Dual Inhibitor of EGFR and ERBB2
Non-small cell lung cancers with activating mutations in the kinase domain of the EGFR demonstrate dramatically, but transient, responses to the reversible tyrosine kinase inhibitors Gefitinib. To identify mechanisms of resistance to Gefitinib, Researchers used NSCLC cells harboring an activating EGFR mutation to generate multiple resistant clones. The bronchoalveolar...
TCH-165, a Proteasome Assembly Modulator, Regulates the Dynamic Equilibrium between the 20S and 26S Proteasome Complexes
Intrinsically disordered proteins (IDPs) involves a number of multiple regulatory and signaling events. In addition, the accumulation of IDPs results in some harmful signals happening in the pathogenesis of many human diseases. The proteasome contains different include active complexes (such as the 26S proteasome) and a weakly active complex: the...