| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| In Vivo | 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: | ||||||||||||
| Name | BIP-135 | ||||||||||||
| CAS | 941575-71-9 | ||||||||||||
| Formula | C21H13BrN2O3 | ||||||||||||
| Molar Mass | 421.24 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |