For research use only. Not for therapeutic Use.
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro[1][2].
Cells treated with Ciliobrevin D exhibits abnormal (unfocused, multipolar, or collapsed) spindles with disrupted γ-tubulin localization in NIH-3T3 cells. Similar Ciliobrevin-induced spindle defects are observed in HeLa cells, although to a lesser extent. Ciliobrevin D addition also reversibly disrupts the pre-formed spindles of metaphase-arrested cells and reduces overall microtubule levels[1]..
Ciliobrevin D reversibly inhibits melanosome aggregation, but the non-cilia-disrupting derivative had no discernible effect at comparable doses. Ciliobrevin D similarly abrogates the movement of peroxisomes in Drosophila S2 cells[1].
Knockdown of Dync1h1 or inactivation of dynein 1 by Ciliobrevin D in the testis in vivo perturbs spermatogenesis. Knockdown of Dync1h1 or the use of Ciliobrevin D to inactivate dynein 1 in the testis in vivo perturbs MT organization through changes in the spatial expression of EB1, perturbs F-actin organization, and perturbs distribution of adhesion protein complexes at the BTB, leading to a loss of BTB integrity. F-actin disorganization in the seminiferous epithelium following Dync1h1 knockdown or dynein 1 inactivation by Ciliobrevin D is mediated by changes in the spatiotemporal expression of actin regulatory proteins Arp3 and Eps8[3].
| Catalog Number | R030628 |
| CAS Number | 1370554-01-0 |
| Synonyms | (Z)-2-(7-chloro-4-oxo-3H-quinazolin-2-yl)-3-(2,4-dichlorophenyl)-3-hydroxyprop-2-enenitrile |
| Molecular Formula | C17H8Cl3N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H8Cl3N3O2/c18-8-1-3-10(13(20)5-8)15(24)12(7-21)16-22-14-6-9(19)2-4-11(14)17(25)23-16/h1-6,24H,(H,22,23,25)/b15-12- |
| InChIKey | HVJSIEVASHGLBF-QINSGFPZSA-N |
| SMILES | C1=CC2=C(C=C1Cl)N=C(NC2=O)C(=C(C3=C(C=C(C=C3)Cl)Cl)O)C#N |
| Reference | [1]. Firestone AJ, et al. Small-molecule inhibitors of the AAA+ ATPase motor cytoplasmic dynein. Nature. 2012 Mar 18;484(7392):125-9. [2]. Miao Y, et al. Dynein promotes porcine oocyte meiotic progression by maintaining cytoskeletal structures and cortical granule arrangement. Cell Cycle. 2017;16(21):2139-2145. [3]. Wen Q, et al. Dynein 1 supports spermatid transport and spermiation during spermatogenesis in the rat testis. Am J Physiol Endocrinol Metab. 2018 Nov 1;315(5):E924-E948. |
