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。
产品描述
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].
体外活性
BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress[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].
体内活性
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. And it does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight)[1].
Cas No.
941575-71-9
分子式
C21H13BrN2O3
分子量
421.24
储存和溶解度
DMSO:56.7mg/mL (134.6mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years