γh2ax

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

L67 (DNA Ligase Inhibitor) is a competitive inhibitor of human DNA ligases I and III with an IC50 of 10 μM.

TopoisomeraseI inhibitor 17 (Compound 7h) is an inhibitor of TopoisomeraseI (Top1). It reduces DDX5 and reverses the locking effect of DDX5 on Top1 activity. This compound induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. It triggers apoptosis by decreasing anti-apoptotic proteins XIAP, Bcl-2, and Survivin, while increasing pro-apoptotic proteins Bax and γH2AX. Moreover, TopoisomeraseI inhibitor 17 halts progression at the G2 M checkpoint, leading to cell cycle arrest. It significantly impairs colorectal cancer cell colony formation and migration, and effectively reduces tumor size in human PDX tumor mouse models.

Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) designed to deliver a topoisomerase I inhibitor (TOP1i). It targets epidermal growth factor receptor (EGFR) and c-MET and demonstrates antitumor activity. The compound induces DNA double-strand breaks, elevates pRAD50 and γH2AX expression, and inhibits the growth of non-small cell lung cancer.

Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.

NSC 80467, a selective DNA damaging agent, functions by inhibiting survivin. Specifically, it preferentially targets DNA synthesis, leading to the induction of two distinct markers of DNA damage, namely γH2AX and pKAP1.

ERCC1-XPF-IN-2 is active in nucleotide excision repair, cisplatin enhancement and γH2AX assays. ERCC1-XPF-IN-2 is a potent inhibitor of ERCC1-XPF endonuclease with an IC 50 value of 0.6 μM [1].