Drug intelligence / Profile preview

ciliobrevin D

Development stage
Unknown
Modality
Small Molecules
01

Overview

Ciliobrevin D is a cell-permeable, reversible, and specific small-molecule inhibitor of the AAA+ ATPase motor cytoplasmic dynein. Discovered through a high-throughput chemical screen for Hedgehog pathway antagonists, Ciliobrevin D targets both cytoplasmic dynein 1 and cytoplasmic dynein 2, blocking their ATPase activity and dynein-dependent microtubule gliding in vitro. By disrupting dynein-mediated retrograde transport, it inhibits primary cilia formation, blocks Hedgehog signaling (preventing the ciliary localization of Gli2 and Smoothened), and perturbs mitotic spindle pole assembly. Ciliobrevin D is widely utilized as a valuable chemical biology tool to investigate dynein-dependent intracellular transport, organelle positioning, and ciliary dynamics in various cellular and developmental models.

Other names
2-(7-chloro-4-oxo-3,4-dihydroquinazolin-2(1H)-ylidene)-3-(2,4-dichlorophenyl)-3-oxopropanenitrileAAA+ ATPase motor cytoplasmic dynein inhibitorCytoplasmic Dynein Inhibitor, Ciliobrevin D
02

Targets

Dynein (Dynein motor family)

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