Drug intelligence / Profile preview

Pan-Ras-In-1

Development stage
Preclinical
Lead developer
Columbia University
Modality
Small Molecules
Administration
Intperitoneal, Intravenous, Oral
01

Overview

Pan-Ras-In-1 (also known as pan-Ras inhibitor 3144 or Compound 3144) is a multivalent, small-molecule pan-RAS inhibitor originally developed by researchers at Columbia University. It binds to multiple RAS isoforms, including wild-type and mutant KRAS, HRAS, and NRAS, with low micromolar affinity, thereby disrupting RAS-effector interactions and downstream MAPK signaling. In preclinical oncology models, Pan-Ras-In-1 exhibits RAS-dependent lethality and suppresses tumor growth in xenograft models of pancreatic cancer, breast cancer, and T-cell acute lymphoblastic leukemia. Beyond its anticancer properties, recent research has demonstrated that Pan-Ras-In-1 possesses potent antibacterial activity against Staphylococcus aureus. It compromises bacterial cell wall integrity by directly binding to the TarA protein (suppressing wall teichoic acid polymer production) and activating CidA-associated peptidoglycan hydrolase systems to induce programmed cell death.

Other names
Pan-RAS-IN-1Pan-RAS-IN1Pan-RAS-IN 1pan-RAS inhibitor-3144
02

Targets

CidA (Holin-like protein CidA)KRAS (Kirsten rat sarcoma viral oncogene homolog)NRAS (Neuroblastoma RAS viral oncogene homolog)RRAS2HRAS (H-Ras protein)TagA (N-acetylglucosaminyldiphosphoundecaprenol N-acetyl-beta-D-mannosaminyltransferase)

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