Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor
Receptor tyrosine kinase FMS like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. The family also includes FMS, kit, and platelet-derived growth factor (PDGF) receptors. Specifically, FLT3 is relevant to regulating the survival, proliferation, and differentiation of hematopoietic stem/progenitor cells. The normal...
Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis
Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...
Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...
UMB298 is a Selective CBP (P300) Bromodomain Inhibitor
CBP (cyclic AMP response element-binding protein) and P300 (E1A binding protein) are two non-BET bromodomain oncology targets. Additionally, P300 is a paralogue of CBP, and they conduct similar activity. Specifically, CBP and P300 are multidomain proteins containing bromodomain and other domains, such as lysine acetyl transferase (KAT). CBP/P300 bromodomains...
AC-4-130 is a Potent STAT5 SH2 Domain Inhibitor
Signal transducer and activator of transcription 5 (STAT5) is a member of the STAT protein family. It is relevant to cell growth and differentiation. Specifically, STAT5 protein has related to cytoplasmic signal transduction and mediates the expression of specific genes. Abnormal STAT5 activity is closely related to a variety...
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...