BIP-135 is a potent inhibitor of glycogen synthase kinase-3 (GSK3) found to be relatively selective for GSK-3β (21 nM) over GSK-3α with modest activity toward PKCβ ( 980 nM; 219 nM), DYRK1B (590 nM), and PI3Kα (870 nM). BIP-135 prolongs the median survival time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. GSK-3 inhibition emerged as an alternative therapeutic target for treating spinal muscular atrophy (SMA) when a number of GSK-3 inhibitors were shown to elevate survival motor neuron (SMN) levels in vitro and to rescue motor neurons when their intrinsic SMN level was diminished by SMN-specific short hairpin RNA (shRNA). References: Chen PC, Gaisina IN, El-Khodor BF, Ramboz S, Makhortova NR, Rubin LL, Kozikowski AP. 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. PubMed PMID: 22348181; PubMed Central PMCID: PMC3279955.

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CAS：941575-71-9