Category: Leukemia

Seliciclib (Roscovitine) is an Orally Active and Selective CDKs Inhibitor

Cyclin-dependent kinases (CDKs) are serine/threonine kinases whose activity depends on a regulatory subunit-a cyclin. Based on the sequence of the kinase domain, CDKs belong to the CMGC group of kinases, along with MAPKs, Gsk3β, DYRK family and CDK-like kinases. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date....

Chelerythrine is a Potent Protein kinase C Inhibitor

Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...

HM43239 is an Orally Active and Selective FLT3 Inhibitor

Acute myeloid leukemia (AML) is the most common acute leukemia in adults, with an incidence of over 20 000 cases per year in the United States alone. Large chromosomal translocations, as well as mutations in the genes involved in hematopoietic proliferation and differentiation, result in the accumulation of poorly...

Tirabrutinib is a Selective BTK Inhibitor

The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...

ABT-737 is a Selective and BH3 Mimetic Bcl-2, Bcl-xL and Bcl-w Inhibitor

Bcl-2 protein family is a key regulator of apoptosis and a marker of B-cell lymphoma. Importantly, apoptosis is an important physiological process of selective cell clearance, involving a variety of biological events. Particularly, the Bcl-2 family is the most characteristic protein family involved in regulating apoptotic cell death. It...

Spautin-1 is a Specific and Potent Autophagy Inhibitor

Autophagy refers to the natural and conservative degradation of cells through lysosome dependent regulation mechanism. Specifically, it allows the orderly degradation and recovery of cellular components. At present, there are four forms of autophagy: macroautophagy, microautophagy, chaperone-mediated autophagy (CMA), and coprophagy. The catabolic process of macroautophagy is evolutionarily conserved...

Daunorubicin is a Topoisomerase II Inhibitor with potent Antineoplastic Activities

Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation...