Category: Acute Myeloid Leukemia

A-674563 is an Orally Active and Selective Akt1 Inhibitor

Akt1 belongs to the Akt subfamily of serine/threonine kinases, which contains the SH2 (SRC homologous 2-like) domain. Specifically, Akt kinase is the central node of the signal transduction pathway, which is important for cell transformation and tumor progression. Besides, Akt is a key mediator of growth factor-induced neuronal survival...

SB-332235 is an Orally Active CXCR2 Antagonist

Chemokines are low m.w. proteins that modulate the immune response through the chemoattraction and activation of leukocytes. These mediators have four classes. Chemokines in which the first two cysteines are separated by a  single,  nonconserved amino acid are CXC or chemokines, while those containing adjacent N-terminalcysteine residues are  CC ...

UZH1a is a Selective METTL3 Inhibitor

METTL3/14 plays a critical role in disorders associated with abnormal self-renewal, aberrant proliferation, and blocking differentiation of hematopoietic cells. Both METTL3 and METTL14 are upregulated in all subtypes of AML, despite the heterogeneity of this blood cell cancer in terms of chromosomal rearrangement and gene mutations. AML and B-cell...

ML390 is a Potent DHODH Inhibitor

Dihydrowhey dehydrogenase (DHODH) catalyzes the fourth enzymatic step of pyrimidine biosynthesis, namely, ubiquinone mediated oxidation of dihydrowhey acid to whey acid. Specifically, DHODH is a mitochondrial protein located on the outer surface of the mitochondrial inner membrane (IMM). Inhibitors of the enzyme are used to treat autoimmune diseases such...

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...