Drug intelligence / Profile preview

raptinal

Development stage
Unknown
Lead developer
University of Illinois
Modality
Small Molecules
Administration
Intraperitoneal, Intravenous
01

Overview

Raptinal is a cell-permeable, small-molecule bifluorene-dicarbaldehyde compound that acts as a rapid and potent inducer of intrinsic pathway caspase-dependent apoptosis. Discovered at the University of Illinois, Raptinal bypasses upstream apoptotic regulators such as BAX, BAK, and BOK to directly trigger mitochondrial outer membrane permeabilization (MOMP) and the subsequent release of cytochrome c into the cytosol, leading to rapid caspase-3 and caspase-9 activation within minutes. In addition to its pro-apoptotic activity, Raptinal has been shown to induce gasdermin E (GSDME)-mediated pyroptosis in certain cancer models, such as melanoma and glioblastoma, and to act as an inhibitor of caspase-activated Pannexin 1 (PANX1) channels. It is widely utilized as a research tool to study cell death pathways and has demonstrated preclinical efficacy in suppressing tumor growth in vivo.

Other names
9H,9'H-9,9'-bifluorene-9,9'-dicarbaldehyde[9,9'-bi-9H-fluorene]-9,9'-dicarboxaldehydeSML1745SML-1745SML 1745
02

Targets

PANX1 (Pannexin-1)

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