72214-67-6

RRD-251 Hydrochloride is a reversible selective disruptor of Rb-Raf-1 interaction.

RRD-251 hydrochloride is a reversiblepotentand selective disruptor of Rb/Raf-1 interaction. The retinoblastoma tumor suppressor protein (Rb) controls the G1-S boundary by repressing the transcriptional activity of the E2F family of transcription factors. Raf-1 kinase binds and phosphorylates Rb early in the G1 phase. RRD-251 significantly inhibits angiogenesis and tumor growth in vivo in an Rb-dependent manner. RRD-251 does not inhibit the binding of B-Raf to Rb and Raf-1 to Mek1/2. AlsoRRD-251 does not affect the kinase activities associated with cyclin Dcyclin E or Raf-1.