bpV (HOpic) is a potent inhibitor of PTEN with an IC50 of 14 nM. The IC50s for PTP-β and PTP-1B are about 350- and 1800-fold higher than the IC50 for PTEN, respectively.
溶解性:Water :69 mg/mL (198.71 mM)
体外研究:
1 μM BpV(Hopic) treatment is capable of increasing the in vitro migration of C2C12 myoblasts, without significantly reducing their ability to differentiate and fuse into multinucleated myotubes. The effects on myoblast migration is in conjuction with enhanced AKT and ERK1/2 signaling.
体内研究:Pharmacological inhibition of PTEN with bpV(HOpic) exacerbates renal dysfunction and promotes tubular damage in mice with IRI(renal ischemia/reperfusion injury) compared with vehicle-treated mice with IRI. PTEN inhibition enhances tubular cell apoptosis in kidneys with IRI, which is associated with excessive caspase-3 activation. Furthermore, PTEN inhibition expands the infiltration of neutrophils and macrophages into kidneys with IRI, which is accompanied by increased expression of the proinflammatory molecules.