Ciliobrevin D 是细胞渗透性,可逆和特异性的 AAA + ATPase 运动细胞质动力蛋白抑制剂。它在体外抑制依赖于动力蛋白的微管滑动和 ATPase 活性。它抑制Hedgehog 信号和初级纤毛形成。
产品描述
Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
体外活性
Ciliobrevin D reversibly inhibits melanosome aggregation, however, the non-cilia-disrupting derivative had no discernible effect at comparable doses. Cells treated with Ciliobrevin D exhibits abnormal (unfocused, multipolar, or collapsed) spindles with disrupted γ-tubulin localization in NIH-3T3 cells. Ciliobrevin D addition also reversibly disrupts the pre-formed spindles of metaphase-arrested cells and reduces overall microtubule levels and it similarly abrogates the movement of peroxisomes in Drosophila S2 cells[1].
体内活性
In the testis in vivo, Knockdown of Dync1h1 or inactivation of dynein 1 by Ciliobrevin D perturbs spermatogenesis. 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[3].
Cas No.
1370554-01-0
分子式
C17H8Cl3N3O2
分子量
392.62
储存和溶解度
DMSO:5 mg/mL (12.73 mM),ultrasonic and warming and heat to 80°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years