Oridonin (Cmpd-5, NSC 250682) is a natural ent-kaurane diterpenoid from Rabdosia rubescens identified as a first-in-class small-molecule inhibitor that directly binds β-arrestin1 and β-arrestin2 with high nanomolar to low micromolar affinity. Oridonin broadly suppresses β-arrestin recruitment, receptor desensitization, internalization, and downstream ERK signaling across multiple GPCR families, and abrogates T-cell chemotaxis.
[1]. Song M, et al. Targeting AKT with oridonin inhibits growth of esophageal squamous cell carcinoma in vitro and patient derived xenografts in vivo. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0823.2017.
[2]. Sun B, et al. Oridonin inhibits aberrant AKT activation in breast cancer. Oncotarget. 2018 Feb 1;9(35):23878-23889.
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