Tag: Low Toxicity

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...

RRx-001 Triggers Apoptosis and Overcomes Drug Resistance in Myeloma

The hypoxic bone-marrow (BM) microenvironment confers growth/survival and drug-resistance in myeloma. Novel therapies via targeting hypoxic-BM milieu may overcome drug resistance. A study from Deepika Sharma Das reported a hypoxia-selective epigenetic agent, RRx-001. In this study, RRx-001 decreases the viability of MM cell lines, as well as overcomes drug-resistance....