Prexasertib dimesylate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. It also inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). This compound induces double-stranded DNA breakage and replication catastrophe, leading to apoptosis, and demonstrates potent anti-tumor activity.
- Selective, ATP-competitive CHK1 inhibitor
- Inhibits CHK1 (Ki 0.9 nM, IC50 <1 nM), CHK2, and RSK1
- Induces double-stranded DNA breakage and replication catastrophe
- Leads to apoptosis and potent anti-tumor activity
- Inhibits MELK, SIK, BRSK2, and ARK5
- Requires CDC25A and CDK2 for DNA damage
- Causes DNA damage during S-phase
- Inhibits CHK1 and CHK2 autophosphorylation
- Induces cell-cycle shift with H2AX phosphorylation
- Triggers chromosomal fragmentation and replication stress