E67-2 is a Selective KIAA1718 Jumonji Domain Inhibitor with Low Toxicity
KIAA1718 is a histone demethylase for repressive methyl marks. what’s more, KIAA1718 involves in transcriptional activation. Specifically, KIAA1718, as a PHF2/PHF8 subfamily member, possesses histone demethylase activity specific for histone H3 lysine 9 (H3K9) and histone H3 lysine 9 (H3K27), transcriptionally repressive histone marks. Furthermore, KIAA1718 forms complexes with...
LP-261 is a Potent and Orally Active Anti-Mitotic Agent
In this article, we will introduce a potent anti-mitotic agent, LP-261. LP-261 shows inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. Firstly, in vitro, LP-261 exhibits potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01 μM to 0.38 μM. Besides, the...
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...
M-808 is a Highly Potent and Efficacious Covalent Menin-MLL Interaction Inhibitor
Menin is a putative tumor suppressor associated with multiple endocrine tumor type 1 (MEN-1 syndrome). Specifically, Menin has two functional nuclear localization signals and inhibits JunD transcriptional activation. MLL1, a histone methyltransferase, is an active global regulator of gene transcription. Besides, the protein belongs to histone-modifying enzyme and contains...
RA-9 is a Selective Proteasome-Associated DUBs Inhibitor
The ubiquitin-proteasome-system (UPS) is responsible for most of the intracellular protein degradation in eukaryotes. UPS consists of three components: the proteasomes, the ubiquitin conjugating system, and the deubiquitinating enzymes (DUBs). DUBs deconjugate ubiquitin from targeted proteins and this step is essential for protein degradation. The de-ubiquitination is required for...
HSD1590 is Potent ROCK Inhibitor with Low Cell Toxicity
Rho-associated protein kinases (ROCKs) are serine-threonine kinases contain isoforms ROCK1 and ROCK2. ROCK1 and ROCK2 exhibit 60% sequence homology and 90% kinase domain homology. The 2 isoforms exist in many organs/tissues but have different expression levels. ROCK1 mainly expresses in thymus, tongue, spleen, and cervix, et al. ROCK2 exists...
AKN-028 is an Orally Active FLT3 Inhibitor
The activation of FMS like receptor tyrosine kinase 3 (FLT3) is a cytokine receptor that belongs to the receptor tyrosine kinase class III. Specifically, FLT3 signaling is important for the normal development of hematopoietic stem cells and progenitor cells. Besides, the FLT3 gene is one of the most common...