RGNCY-0106 (RIN1 RBPJ inhibitor)
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RIN1 is a novel inhibitor that disrupts NOTCH and RBPJ interaction which is the main transcriptional effector of NOTCH signalling. RIN1 also blocked the functional interaction between RBPJ and SHARP, a scaffold protein that forms a transcriptional repressor complex with RBPJ in the absence of NOTCH. Importantly, RIN1 induces gene expression changes similar to siRNA silencing of RBPJ rather than inhibition of NOTCH itself. Thus, RIN1 inhibited hematologic cancer cell line proliferation and promoted skeletal muscle differentiation from C2C12 myoblasts.
Systematic Name: 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)benzamide
SMILES: CN1N=CC=C1C2=CC(OC3=CC=CC=C3F)=C(C(N)=O)C=C2
Formula: C17H14FN3O2
Mol Wt: 311.32
PMID: 31346210
Tags: Small molecules, Cancer, RGNCY-0106, RIN1, RBPJ, NOTCH, SHARP, hematologic