TAS-119 is a Selective and Orally Active Aurora A Inhibitor
Aurora kinases represent a serine/threonine kinase family crucial for cell-cycle control. In particular, Aurora kinases are important and indispensable in multiple steps of mitotic progression. Specifically, Aurora kinase A acts primarily during the prophase of mitosis. Overexpression of Aurora A in HeLa cells attenuates the antiproliferative activity of Paclitaxel....
MK-2206 is an Orally Active and Selective Allosteric Akt Inhibitor
Nasopharyngeal carcinoma (NPC) is a squamous cell carcinoma arising from the epithelium lining of the posterior nasopharynx. In a word, NPC causes very serious health problems in these areas. NPC is highly sensitive to radiation and chemotherapy. However, even with combined radiation and chemotherapy treatment, the prognosis for the...
ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader
Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....
HKI-357 is an Irreversible Dual Inhibitor of EGFR and ERBB2
Non-small cell lung cancers with activating mutations in the kinase domain of the EGFR demonstrate dramatically, but transient, responses to the reversible tyrosine kinase inhibitors Gefitinib. To identify mechanisms of resistance to Gefitinib, Researchers used NSCLC cells harboring an activating EGFR mutation to generate multiple resistant clones. The bronchoalveolar...
CP5V is a Specific PROTAC Degrader of Cdc20
The cell-division cycle protein 20 (Cdc20) is the substrate receptor of anaphase synthesis complex (APC) or cyclosome (APC/C). Besides, it coordinates late initiation and exit of mitosis through safety and time-dependent degradation. Cdc20 is a key mitotic factor, which controls the beginning of anaphase and the exit of mitosis....
SCH772984 is an ATP Competitive and Non-Competitive ERK1 and ERK2 Inhibitor
Specific inhibitors of RAF and MEK kinases to target BRAF– and RAS-mutant tumors are developing. Interestingly, BRAF/MEK inhibitor combination treatment blocks phosphorylated extracellular signal-regulated kinase (phospho-ERK) reactivation in melanoma cells, a phenomenon that may possibly reduce the emergence of clinical resistance. ERK represents an attractive downstream target to exploit. SCH772984...
YUKA1, a Specific KDM5A Inhibitor, Inhibits Drug Resistance
KDM5A (Lysine-specific demethylase 5A) is a histone lysine demethylase, which binds with other proteins to retinoblastoma protein. The latter regulates cell proliferation. KDM5A exhibits high levels of some human cancers. It involves cancer processes, such as tumorigenesis, metastasis, and drug tolerance. Therefore, we need to found out more KDM5A...