PD 168368

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the K_i of 15–45 nM^[1]. PD 168368 is neuromedin B receptor (NMBR; IC₅₀=96 nM) / gastrin-releasing peptide receptor (GRPR IC₅₀=3500 nM) antagonist^[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC₅₀s of 0.57, 0.24, and 2.7 nM, respectively^[3]. In Vitro: PD 168368 (PD168368) is highly active and stimulated [Ca²⁺]_I release in human neutrophils with EC₅₀ values in the nanomolar range^[3].
PD 168368 (PD168368) suppresses migration and invasion of the human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation. PD 168368 (5 μM) inhibits migration and invasiveness in breast cancer cells^[4].
PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells^[4]. In Vivo: PD 168368 (PD168368) potently inhibits in vivo metastasis of breast cancer. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits metastasis of breast cancer in mice^[4].