BIP-135 是一个高效、选择性的，ATP 竞争性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 作用的IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect[1].
BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations[1].BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress[1]. Western Blot Analysis[1] Cell Line: Human SMA fibroblasts
BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight)[1].BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of δ7 SMA KO mouse model of spinal muscular atrophy[1]. Animal Model: Male and female SMN2+/+, SMN2δ7+/+, Smn+/- mice[1]
[1]. Chen PC, et al. Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.
动态评分
0.0