Medchemexpress LLC Prexasertib (dimesylate) | 1234015-58-7 | 98.9% | 557.60 | 5 MG

Supplier:  Medchemexpress LLC HY18174E5MG

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

Catalog No. 50-003-87525