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.
体外研究
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.
BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress.
Western Blot Analysis
Cell Line:
Human SMA fibroblasts
Concentration:
20 μM, 25 μM, 30 μM
Incubation Time:
72 hours
Result:
Led to a 7-fold increase in SMN levels at 25 μM.
体内研究
BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight).
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.
Animal Model:
Male and female SMN2, SMN2Δ7, Smn mice
Dosage:
75 mg/kg
Administration:
Intraperitoneal injection; daily; from postnatal day 0 to 21
Result:
Caused a modest extension in the median survival of SMA KO animals by two days.
分子式
C21H13N2O3Br
分子量
421.24
CAS号
941575-71-9
运输条件
Room temperature in continental US; may vary elsewhere.