Month: August 2022

BNS-22 is a DNA Topoisomerase II Catalytic Inhibitor

Topoisomerases (DNA topoisomerases) are enzymes that catalyze changes in the topological state of DNA, regulating the overwinding or underwinding of DNA. Topoisomerases play essential roles in DNA replication, transcription, chromosome segregation, and recombination. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. All...

BI-1622 is an Orally active and Selective HER2 Inhibitor

BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, with IC50 values of 7.8, 7.1, <5.3 nM for HER2WT, HER2YVMA, EGFRWT, respectively. Besides, BI-1622 shows greater than 25-fold selectivity over EGFR. Moreover, BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models. HER2 is a member...

PU-H54, a Grp94-selective Inhibitor, Can be Used for Breast Cancer Research

Heat shock proteins (HSPs) are a family of proteins produced by cells in response to exposure to stress conditions. Besides, HSPs are a large class of molecular chaperones. It plays a role in protein maturation, refolding, and degradation. Moreover, HSPs may promote or inhibit neural development by regulating cell...

KGP94 is a Selective Inhibitor of Cathepsin L for Cancer Research

Cathepsin L is a lysosomal cysteine protease. Particularly, it may play a key role in various biological and disease processes through intracellular and extracellular protein degradation. Obviously, cathepsin L is a ubiquitously expressed cysteine protease located in lysosomes under normal conditions. However, cancer cells secrete cathepsin L to help...

ML-097 (CID-2160985) is a Pan Ras-related GTPases Activator

Ras, is a family of related proteins expressed in all animal cell lineages and organs. All Ras protein family members belong to a class of protein called small GTPase. Furthermore, Ras is a prototypical member of the Ras protein superfamily that regulates a variety of cellular behaviors. As a...

Rucaparib (AG014699) is an Orally Active PARP-1/2/3 Inhibitor

Poly (ADP-ribose) polymerase (PARP), a family of proteins, is involved in various cellular processes such as DNA repair and programmed cell death. PARP presents in the cell nucleus. It consists of a DNA-binding domain, a caspase-cleaved domain, an auto-modification domain, and a catalytic domain. In particular, the protein can...