UBS109

Most water soluble synthetic monocarbonyl analog of curcumin (MAC) for in vitro and in vivo application. Potently inhibits NF-kappaB and its nuclear translocation by suppressing IKK-alpha and IKK-beta, consequently leading to apoptosis. Potent DNA hypomethylating agent. Inhibits HSP90 and NF-kappaB leading to downregulation of DNA methyltransferase-1 (DNMT-1) expression. Cytotoxic against several cancers in vitro and in vivo. Shows excellent activity against xenografts of head and neck squamous cell carcinoma, pancreatic cancer, colon cancer and breast cancer. Antiangiogenic agent. Induces the downregulation of HIF-1alpha, HSP90, COX-2 and VEGF in tumor samples from xenograft models compared to untreated xenografts. Shows preventive effects on bone loss induced by breast cancer cell bone metastasis. Found to have a potential stimulating effect on osteoblastogenesis and a suppressive effect on osteoclastogenesis in vitro through Smad activation and NF-kappaB inhibition. May have promise in the development into an antiosteoporotic agent capable of promoting new bone formation while simultaneously reducing bone resorption.