Application

HLM006474 has been used as an E2 factor(E2F) inhibitor in human nasopharyngeal carcinoma hone-1 cells and T. annulata-infected TBL20 cells.

Biochem/physiol Actions

HLM006474 is a pan-E2F transcription factor inhibitor. E2F s part of the CDK/Rb/E2F pathway. When phosphorylated by CDKs, the tumor suppressor retinoblastoma protein (Rb) is inactivated, releasing E2Fs and allowing cell cycle progression. HLM006474 inhibited DNA-binding of all E2F complexes and down-regulated expression of E2F4 protein. HLM006474 induced apoptosis of A375 melanoma cells and synergized with paclitaxel in lung cancer cell lines.

HLM006474 activates p53 and induces DNA damage and apoptosis in mouse tumor models.

Packaging

5, 25 mg in glass bottle