rks-262

RKS262 is a specific cyclin CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

E09241 is a novel OPG RANKL upregulator, increasing OPG expression without affecting RANKL expression, promoting osteoblast differentiation while inhibiting osteoclast differentiation, regulating OPG expression through canonical Wnt β-catenin signaling.