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Dynarrestin is a novel inhibitor of cytoplasmic Dyneins 1 and 2, acts reversibly to inhibit cytoplasmic dynein 1-dependent microtubule binding and motility in vitro without affecting ATP hydrolysis; rapidly and reversibly inhibits endosome movement in living cells and perturbs mitosis by inducing spindle misorientation and pseudoprometaphase delay; reversibly inhibits cytoplasmic dynein 2-dependent intraflagellar transport (IFT) of the cargo IFT88 and flux of Smo within cilia without interfering with ciliogenesis and suppresses Hh-dependent proliferation of neuronal precursors and tumor cells.


Ciliobrevin D


Ciliobrevin D is a cell-permeable, reversible, specific inhibitor of cytoplasmic dynein, blocks dynein-dependent microtubule gliding and ATPase activity while sparing kinesin dependent cellular trafficking; selectively affects retrograde transport, inhibits the bidirectional transport of organelles along sensory axons and impairs NGF-mediated regulation of growth cones and axon branches, disrupts spindle pole focusing and kinetochore-microtubule attachment at 10-40 uM



1823133-56-7 Dynein2-IN-37 (Ciliobrevin analog 37) is a potent, selective cytoplasmic dynein 2 ATPase activity antagonist with IC50 of 11 uM, shows weak inhibition for dynein 2 (IC50=280 uM); directly targets the heavy chains of both dynein isoforms and explore the structure-activity landscape of these inhibitors in vitro and in cells; inhibits retrograde ciliary GLI2 transport more strongly than ciliobrevin A, effectively disrupts Hedgehog signaling, intraflagellar transport, and ciliogenesis.

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