Month: August 2020

YKL-5-124 is a Selective, Irreversible and Covalent CDK7 Inhibitor

Cyclin-dependent kinase 7 (CDK7) is a member of the cyclin-dependent protein kinase (CDK) family. Specifically, CDK7 is an important component of TFIIH, which is involved in transcription initiation and DNA repair. Besides, CDK7 protein is a direct link between transcriptional regulation and cell cycle. In the cytoplasm, CDK7 contains...

JH295 is an Irreversible and Selective NIMA-Related Kinase 2 (Nek2) Inhibitor

NIMA-related kinase 2 (Nek2) is a homodimeric serine/threonine kinase. It localizes to centrosomes, the microtubule organizing centers of the cell. At the onset of mitosis, Nek2 phosphorylates the inter-centrosome linker proteins, C-Nap1, and rootletin. Nek2 plays a role in bipolar spindle assembly driven by the microtubule motor protein, Eg5....

BM-1197 is a Potent and Selective Dual Bcl-2/Bcl-xL Inhibitor

Bcl-2 and Bcl-xL are critical regulators of apoptosis. The pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising strategy for cancer treatment. In addition, BM-1197 is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL. BM-1197 binds to Bcl-2 and Bcl-xL proteins with Ki values less than 1...

SBP-0636457, a SMAC Mimetic, is an IAP Antagonist

Cancer cells regularly acquire resistance to programmed cell death, or apoptosis, which not only supports cancer progression but also leads to resistance to therapeutic agents. In this study, researchers focus their research on the inhibitor of apoptosis protein (IAP) family. IAPs are a disparate group of proteins that all...

SP-146 is a Selective and non-ATP-Competitive Aurora B Inhibitor

Aurora B Kinase is a serine-threonine kinase and plays an important role in mitosis. This kinase also plays an important role in mitosis as a serine-threonine kinase. It also a part of the chromosomal passenger complex (CPC).  Overexpression of Aurora B has been reported in several cancers, such as...