TK4g is a JAK Inhibitor for Leukemia Cancer Research
Janus kinase (JAK) is an intracellular non-receptor tyrosine kinase. There are four members of the JAK family: JAK1, JAK2, JAK3, and Tyrosine kinase 2 (TYK2). JAK can link cytokine signals from membrane receptors to activators of transcription (STAT), transducing cytokine-mediated signals via the JAK-STAT signaling pathway. When the receptor...
Pulrodemstat is a Potent, Selective, Reversible and Orally Active Inhibitor of LSD1
Lysine-specific histone demethylase 1A (LSD1) also known as lysine (K)-specific demethylase 1A (KDM1A) is a protein in humans that is encoded by the KDM1A gene. LSD1 is a member of a broad family of monoamine oxidases that requires FAD as a cofactor to catalyze demethylase activity. In addition, LSD1...
Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I
Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116...
5-Azacytidine, a Nucleoside Analogue of Cytidine, Inhibits DNA Methylation
In the mammalian genome, DNA methylation is an epigenetic mechanism involving the transfer of a methyl group onto the C5 position of the cytosine to form 5-methylcytosine. DNA methylation regulates gene expression by recruiting proteins involved in gene repression or by inhibiting the binding of transcription factor(s) to DNA....
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...
Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor
Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...
Flavopiridol (Alvocidib) is a pan CDK Inhibitor
The cyclin-dependent kinases (CDKs) are serine/threonine protein kinases. And it exhibits drives force behind the cell cycle and cell proliferation. CDKs contain at least a catalytic subunit (CDK) and a regulatory subunit (cyclin). To date, at least 10 CDKs and 15 cyclins have been identified. Once activation, CDKs phosphorylate...