Tag: Low Toxicity

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...

BCI-215 is a Tumor Cell-Selective DUSP-MKP Inhibitor

Mitogen-activated protein kinase phosphatases (MKPs) belongs to the dual-specificity phosphatase (DUSP) family. DUSP-MKPs dephosphorylate and inactivate the MAPKs extracellular signal-regulated kinase (ERK), JNK/SAPK, and p38 on tyrosine and threonine residues. As a result, they result in regulating the duration and amplitude of mitogenic and survival signaling. There exists a ...

CSRM617 is a Transcription Factor ONECUT2 Inhibitor for Prostate Cancer

The transcription factor ONECUT2 (OC2) is a master regulator of androgen receptor networks in mCRPC (metastatic castration-resistant prostate cancer ). OC2 acts as a survival factor in mCRPC models. OC2 is a potential drug target in the metastatic phase of aggressive PC. CSRM617,  a well-tolerated novel small-molecule inhibitor of...