Category: Acute Myeloid Leukemia

SKI-178 is a Potent SphK1 and SphK2 Inhibitor

Sphingosine kinase (SphK) is an oncogenic lipid kinase and a key regulator of the sphingolipid metabolic pathway. The SphK isoforms (SphK1 and SphK2) catalyze the conversion of the pro-apoptotic substrate D-erythro-sphingosine (Sph) to the pro-growth/survival product sphingosine-1-phosphate (S1P). In addition, over-expression of SphK1/SphK2, have been associated with oncogenic transformation...

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...

GSK621 is a Specific AMPK Activator, Inducing Autophagy and Apoptosis

AMPK is an enzyme, which plays a role in cell energy homeostasis. It mainly activates glucose and fatty acid uptake and oxidation when the cell energy is low. Specifically, AMPK is a major regulator of cell metabolism, which can exert its carcinogenic or antitumor activities. Besides, the activation of...

THZ-P1-2 is a Selective PI5P4K Inhibitor

Phosphatidylinositol 5-phosphate (PI-5-P) is one of the seven phosphoinositides. They regulate a wide range of cellular functions. They localize in the nucleus, Golgi, endoplasmic reticulum, and at the plasma membrane. PI-5-P is an oxidative stress-induced regulator of AKT activation. The phosphorylation of the low abundance phosphoinositide PI-5-P at the...

OT-82 is an Orally Active NAMPT Inhibitor with Antineoplastic Activity

Treatment of hematopoietic (HP) malignancies such as leukemia, lymphoma, and myeloma need improvement due to the drug high toxicity. Some effective anticancer agents are tissue-selective but not cancer-specific targets. These agents cannot distinguish normal and transformed cells. Besides they are usually against lineage-specific metabolic deficiency or lineage-specific surface antigen,...

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...

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...