PD 168368

Research use only, not for human use.

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.

PD 168368 (PD168368) is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range. 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.PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells.Cell Viability Assay Cell Line:Human breast cancer cell line MDA MB-231 Concentration: 5 μM Incubation Time:24 hours Result:Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay.Cell Viability Assay Cell Line:MDA-MB-231 cells Concentration:10 μM Incubation Time:0, 0.5, 1, 2, 4, 8, and 16 hours Result:Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner.

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.Animal Model:Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model Dosage:1.2 mg/kg Administration:Intraperitoneal injection for 30 days Result:No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice.

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GPCR/G Protein

Bombesin Receptor

Bombesin Receptor

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204066-82-0

554.64

C31H34N6O4

>98% (HPLC)

In Vitro:?DMSO : 30 mg/mL (54.09 mM) DMF : 10 mg/mL (18.03 mM)

C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(cc1)[N+]([O-])=O)C(=O)NCC1(CCCCC1)c1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years