CC-90011 is a Selective and Orally Active Inhibitor of LSD1
Lysine-specific histone demethylase 1 (LSD1) (also known as KDM1) is a member of a broad family of monoamine oxidases and is encoded by the KDM1A gene. However, LSD1 requires the flavin adenine dinucleotide (FAD) as a cofactor to catalyze demethylase activity. For example, LSD1 catalyzes demethylation at H3K4me1/2 and...
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...