ABT-737 is a Selective and BH3 Mimetic Bcl-2, Bcl-xL and Bcl-w Inhibitor
Bcl-2 protein family is a key regulator of apoptosis and a marker of B-cell lymphoma. Importantly, apoptosis is an important physiological process of selective cell clearance, involving a variety of biological events. Particularly, the Bcl-2 family is the most characteristic protein family involved in regulating apoptotic cell death. It...
Crizotinib is an Orally Active, ATP-Competitive ALK and c-Met inhibitor
In this article, we will introduce an orally bioavailable, ATP-competitive ALK and c-Met inhibitor, Crizotinib. The IC50 values for ALK and c-Met kinases are 20 and 8 nM, respectively. Additionally, in cell-based assays, Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM, respectively. In...
Pelcitoclax (APG-1252) is a Bcl-2/Bcl-xl Inhibitor with Antineoplastic and Pro-Apoptotic Effects
Bcl-2 (B-cell lymphoma 2) is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). Particularly, the Bcl-2 and Bcl-xl...
SIS3 is a Potent and Selective Inhibitor of Smad3 Phosphorylation
Smad contains a series of proteins with similar structures, which are the main signal transducer in transforming growth factors β (TGF-b) superfamily. Specifically, they play an important role in the regulation of cell development and growth. One mechanism of Smads promoting TGF-b-induced cell arrest is down-regulation of Myc, a...
CPL304110 is an Orally Active and Selective FGFR(1-3) Inhibitor
Over the last decade, the FGFRs family has become an attractive validated therapeutic target notably in cancer. It consists of four members (FGFR1 to FGFR4) which are structurally related cell surface RTKs. This FGF-FGFR axis participates in key biological processes that play significant roles in cell functions such as...
BAY1082439 is an Orally Active and Selective Balanced PI3Kα/β/δ Inhibitor
Prostate cancer is among the most common malignancy in males. Among the various PI3K isoforms, PTEN-loss-induced prostate cancer in the genetically engineered Pten conditional knockout mouse model predominantly activates the PI3Kβ subunit. However, selective inhibition of PI3Kβ shows no significant anti-tumor efficacy in PTEN-null prostate cancer cell lines. It...
LCH-7749944 is a Potent PAK4 Inhibitor and Induces Apoptosis
P21-activated kinase 4 (PAK4) is a serine/threonine protein kinase and has related to the regulation of cytoskeleton recombine, cell proliferation, gene transcription, carcinogenic transformation, cell invasion. Moreover, PAK4 overexpression, mutations, genetic amplification were detected in a variety of human tumors, making it a potential therapeutic target. Specifically, The p21-activated kinases...