2682114-39-0

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation[1].

RBPJ Inhibitor-1 (RIN1) is a selective inhibitor against the transcription factor RBPJ. RIN1 blocks RBPJ-SHARP transcriptional repressor complex formationinhibits RBPJ-mediated Notch intracellular domain (NICD) transcription activity (IC50/Emax = 180 nM/82% and 190 nM/88% using Notch2 ICD or Notch3 ICDrespectively)as well as NICD-independent transcription activity of RBPJ-VP16 (IC50 = 200 nMEmax = 81%). RIN1 inhibits Notch-driven cancer proliferation (by ~70% post 4-day 10 μM RIN1 treatment; Jurkat) and promotes muscle differentiation (0.6 μM for 4 days; C2C12 myoblasts).

[1] Cecilia Hurtado, et al. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci Rep. 2019 Jul 25;9(1):10811. DOI:10.1038/s41598-019-46948-5