BTSA1 is a High Affinity and Orally Active BAX Activator
The BCL-2 family protein BAX is a central mediator of apoptosis. Besides, overexpression of anti-apoptotic BCL-2 proteins contributes to tumor development and resistance to therapy by suppressing BAX and its activators. Cancer cells depend on their ability to enforce cell survival pathways and block cell death mechanisms. Moreover, pro-apoptotic...
A-366 is a Potent Histone Methyltransferase G9a Inhibitor
Epigenetic alterations to the genome take place via modifications to the DNA or histones. Meanwhile, those modifications lead to changes in gene expression. Generally, histone lysine methylation is a prominent kind of epigenetic regulation for change of the structure chromatin and gene expression. HMTs have recently generated increasing interest...
PI-103 is a Potent PI3K and mTOR Inhibitor
The phosphatidylinositide 3-kinase family possesses 15 members. those members consist of four distinct classes as a basis on their structure and biological properties. As we all know, this highly conserved family of enzymes involves various aspects of cellular homeostasis and exists a decline in a number of pathophysiologic conditions....
SD-36 is a Selective PROTAC STAT3 Degrader
Proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. In this study, Longchuan Bai, et al developed a potent and specific PROTAC degrader of STAT3 and evaluate its...
ASLAN003 is an Orally Active hDHODH Inhibitor
Dihydroorotate dehydrogenase (DHODH) is a highly conserved enzyme. All organisms express it. Class-1 DHODHs are cytoplasmic and single-domain enzymes. Conversely, class-2 DHODHs are membrane-associated and two-domain enzymes. Both classes of DHODHs use FMN to oxidize DHODH. To regenerate FMN, class-1 enzymes use a soluble cofactor, such as NAD+ or fumarate,...
PTC596 is an Orally Active and Selective BMI-1 Inhibitor
BMI-1 is a highly conserved class II member of the Polycomb group of genes, regulating diverse aspects of transcription, stem cell maintenance, cell proliferation, and oncogenesis. BMI-1 has vital functions in the self-renewal and maintenance of AML and normal hematopoietic stem cells. The first BMI inhibitor PCT-209 has a...
TL02-59 is a Selective and Orally Active Myeloid Src-family Kinase Fgr Inhibitor
Acute myelogenous leukemia (AML) is a devastating hematologic cancer with limited treatments. Scientists have demonstrated that diverse genetic changes are associated with AML. Especially, the upregulation of tyrosine kinase signaling pathways stands for a common feature. Additionally, mutations in the Flt3 receptor tyrosine kinase accounts for almost one-third of...