Dynapyrazole-A

Dynapyrazole-A is an inhibitor of the motor proteins dynein 1 and dynein 2. It inhibits the microtubule-stimulated ATPase activity of dynein but not its basal microtubule-independent activity. Dynapyrazole-A inhibits dynein 1- and dynein 2-mediated microtubule gliding in a cell-free assay (IC50s = 2.3 and 2.6 µM, respectively). It also inhibits hedgehog pathway stimulation induced by SAG (Cay11914) in a reporter assay using NIH3T3 cells (IC50 = 1.9 µM). Dynapyrazole-A (10 µM) reversibly reduces the speed of intraflagellar retrograde and, to a lesser extent, anterograde transport in mouse inner medullary collecting duct (mIMCD-3) cells. It also reduces lysosomal transport in catecholamine A-differentiated (CAD) cells.. SMILES: N#CC(C(C1(CC1)C2=CC=C(C=C2)Cl)=NN3C4=CC=C(C=C45)I)=C3NC5=O. InChi Code: InChI=1S/C20H12ClIN4O/c21-12-3-1-11(2-4-12)20(7-8-20)17-15(10-23)18-24-19(27)14-9-13(22)5-6-16(14)26(18)25-17/h1-6,9H,7-8H2,(H,24,27). InChi Key: VABPBCMFKJDOHP-UHFFFAOYSA-N