Category: Cancer

NSC-105808 is a Specific DNA2 Nuclease Inhibitor with Antitumor Activity

DNA2 nuclease possesses 5′ flap endonuclease and 3′-5′ helicase activities. It has an important role in DNA damage repair, homologous recombination, and DNA replication. The nuclease activity of DNA2 has several well-documented cellular functions. However, the biological role of its helicase activity remains enigmatic. DNA2 mediates the resection of...

R59949 is a pan Diacylglycerol Kinase (DGK) Inhibitor

Diacylglycerol kinase (DGK) is a second messenger in its own right and can modulate the activity of PKC and several ion channels.  Chemokines are low MW extracellular signaling peptides secreted by tissue either constitutively during homeostasis or de novo during an inflammatory response. They are a diverse family of...

WL47 is a Selective, High-Affinity, Disrupter of Cavolin-1 Oligomers

The family of caveolin membrane proteins plays many roles in the cell’s structural, signaling, and transportation processes. Caveolin-1 (CAV) is a monotonic membrane protein, 22 kDa, it penetrates only one leaflet of the lipid bilayer, and both the N- and C-termini remain on the cytoplasmic side. Multiple copies of CAV oligomerize...

CHDI-390576 is a CNS Penetrant Class IIa HDAC Inhibitor

Class IIa HDAC is a transcriptional corepressor enzyme. They interact with MEF2 transcription factors and the N-CoR, BCoR, and CtBP corepressors.  They are capable of shuttling between the cytoplasm and nucleus, hence they are directly linked to cellular signaling networks. Class IIa HDACs found in a wide variety of...

ML132 is a Potent and Selective Caspase 1 Inhibitor

Caspases are cysteine proteases with strict specificity for cleaving peptide sequences C-terminal to aspartic acid residues. A prominent member of the pro-inflammatory class is caspase 1. It is responsible for the proteolytic activation of interleukin (IL)-1β and IL-18. IL-1β and IL-18 are cytokines. They play a major role in...

ZXH-3-26 is a Selective PROTAC BRD4 Degrader

Targeting protein degradation refers to small molecule induces ubiquitination and degradation of disease targets. These small molecules simultaneously recruit both a ubiquitin E3 ligase and the target protein, then to be ubiquitinated. Therefore, PROTACs represent a functional application of chemically induced protein dimerization. BRD4 acts as an attractive target...