GSK778 is a Potent and Selective Inhibitor of BET BD1
The bromodomain is a protein domain of about 110 amino acids, which can recognize acetylated lysine residues. Specifically, the bet (Bromo- and terminal domain) family consists of germ cell-specific (BRDT) and ubiquitously expressed (BRD2, BRD3, Brd4) epigenetic reader proteins. As a “reader” of lysine acetylation, bromodomain is responsible for...
AMG-458 is a Selective and Orally Bioavailable c-Met Inhibitor
C-met is a protein encoded by a met gene in humans, which has tyrosine kinase activity. Specifically, Met is an essential one-way tyrosine kinase receptor for embryonic development, organogenesis, and wound healing. Besides, C-met is a receptor tyrosine kinase that can be activated by its ligand, hepatocyte growth factor/dispersion...
EW-7195 is a Specific ALK5 (TGFβR1) Inhibitor with Anti-Metastasis Activity
Breast cancer is the leading cause of cancer mortality among women in Korea, England, and the United States of America. Invasion and metastasis are the most lethal characteristics of breast cancer. TGF-β signaling maintains homeostasis and elicits tumor-suppressive responses such as growth inhibition and apoptosis in normal mammary epithelial...
SR7826 is a Selective and Orally Active LIM kinase (LIMK) Inhibitor
LIM-kinase (Limk) is a serine-threonine protein kinase. Two isoforms are LIM kinase 1 (Limk1) and LIM kinase 2 (Limk2). Limk1 is overexpressed in cancerous prostate cells and tissues. Previous studies shows that the possibility of up-regulated Limk1 as a cellular oncogene and inhibition of Limk1 activity in cancerous prostate...
TAI-1 is an Orally Active and Highly Potent Hec1 Inhibitor
Hec1 (Ndc80) is one of the outer kinetochore proteins and forms heterotetramers with proteins NUF2, SPC25, and SPC24. Specifically, drugs that interfere with mitosis are part of the most successful chemotherapeutic compounds for cancer in clinical practice. Hec1, a component of mitochondria, is overexpressed in a variety of human...
MRK-740 is a Selective and PRDM9 Histone Methyltransferase Inhibitor
PRDM9 is a zinc finger protein that binds DNA at specific locations in the genome and alleles influence human chromosomal rearrangements, causing hereditary diseases. MRK-740 is a potent selective and cell-active PRDM9 inhibitor with an IC50 of 80 nM. In cells, MRK-740 specifically and directly inhibits H3K4 methylation at endogenous...
RA375, a RPN13 Inhibitor, Activates UPR Signaling, ROS Production and Apoptosis
Rpn13 is a known component of the proteasome. Especially, Rpn13 binds ubiquitin-like domains of the UBL/UBA family of ubiquitin receptors. Rpn13, as an ubiquitin receptor, offers a docking position for ubiquitinated substrate. RA375 is a RPN13 inhibitor. Treatment with RA375 causes a rapid and profound accumulation of high molecular weight polyubiquitinated proteins. RA375...