Stemcell, 100-1169, Olaparib

Inhibit cancer cell growth by selectively inhibiting poly ADP ribose polymerase (PARP) with olaparib. With a high affinity for both PARP1 and PARP2 (IC50 = 5 and 1 nM), olaparib is an inhibitor of PARPs in cancer cells with BRCA1 or BRCA2 mutations (Menear et al.). PARPs are a family of enzymes that repair DNA breaks by assisting with base excision repair (BER); olaparib inhibits this activity, leading to DNA damage and cell death (Davar et al.).

Olaparib has been used for:

CANCER RESEARCH

· Inhibits tumor growth and overall survival in ATM-deficient mantle cell lymphoma cells (Williamson et al.).

· Inhibits growth of esophageal squamous cell carcinoma cells by cell cycle arrest at G2/M (Nasuno et al.).

· Induces anti-proliferative effects in specific endometrial cancer cell lines (Miyasaka et al.).

· Reported as a potentially effective therapeutic agent against epithelial ovarian cancer (Chen & Du).

· Prevents or partially reverts epithelial-mesenchymal transition (EMT) induced by TGF-β in NMuMG cells (Schacke et al.).

· Reported to prevent OVA-induced airway inflammation and remodeling through modulation of inflammasome signaling in mice (Sethi et al.).