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 (β1: 980 nM; β2: 219 nM), DYRK1B (590 nM), and PI3Kα (870 nM). BIP-135 was found to be a superior neuroprotective agent in a cortical neuron model of oxidative stress over other GSK-3 inhibitors, such as AR-A011418 and SB216763. In a mouse model of spinal muscular atrophy (SMA), BIP-135 elevated SMN protein levels in vitro and extended median survival.
Glycogen synthase kinase 3 (GSK-3) is a highly conserved family of serine/threonine kinases for over 100 proteins in many pathways. See a list of accepted GSK-3 modulators and related products.
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