h2ax

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

RHPS4 (RHPS 4 methosulfate) is a potent inhibitor of Telomerase at submicromolar.

Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase/Akt pathway, promotes histone H2AX phosphorylation, and induces G2/M arrest in the cell cycle.

BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

FMP is a platinum (IV) complex. It significantly upregulates the expression of γ-H2AX and p53, enhances ROS production, and markedly increases the expression of apoptosis (Apoptosis) related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP exhibits antiproliferative activity against breast cancer.

S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem

SFOM-0046 is an anticancer agent. SFOM-0046 arrests the cell cycle in S-phase and causes DNA replication stress, resulting in the phosphorylation of H2AX into gamma-H2AX.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.

OTS186935 hydrochloride is a potent inhibitor of the protein methyltransferase SUV39H2 (IC50: 6.49 nM). oTS186935 hydrochloride significantly inhibited tumor growth in a mouse xenograft model with no apparent toxicity. oTS193320 OTS193320 hydrochloride was able to modulate γ-H2AX production in cancer cells.

Antitumor agent-37 exhibits potent anti-proliferative and anti-metastatic effects. antitumor agent-37 induces severe DNA damage, leading to high expression of γ-H2AX and p53. antitumor agent-37 induces apoptosis by exploiting the mitochondrial apoptosis pathway Bcl-2 Bax caspase3. Antitumor agent-37 inhibits PD-L1 expression, increases CD3+ and CD8+ T-infiltrating cells in tumour tissue and significantly improves the immune response.

OTS193320, an imidazopyridine compound, acts as an inhibitor of SUV39H2 methyltransferase activity. It effectively reduces global histone H3 lysine 9 tri-methylation levels in breast cancer cells, promoting apoptotic cell death. When combined with Doxorubicin (DOX), OTS193320 enhances the reduction of γ-H2AX levels and decreases cancer cell viability more significantly than when either agent is used alone.

Antitumor agent-36 exhibits strong anti-proliferative and anti-metastasis capabilities, causing significant DNA damage that results in elevated levels of γ-H2AX and p53. It promotes tumor cell apoptosis via the mitochondrial apoptotic pathway involving Bcl-2 Bax caspase3 and enhances immune response by inhibiting PD-L1 expression, thereby increasing CD3+ and CD8+ T cell infiltration in tumor tissues [1].