Spastazoline

Spastazoline is an inhibitor of spastin (IC50 = 99 nM for the human enzyme). It is selective for spastin over a panel of 64 kinases but does inhibit tropomyosin-related kinase A (TrkA) by 65% at 2 µM. Spastazoline (10 µM) increases the number of cells with intracellular bridges during cell division, indicating microtubule stabilization, in HeLa cells expressing the recombinant human M87 isoform of spastin that contains the alternatively spliced exon 4 (M87e4). It inhibits neurite outgrowth in primary mouse hippocampal neurons when used at concentrations of 1 and 5 µM. Spastazoline (20 mg/kg, i.p.) increases spinal cord injury-induced motor impairments in mice, but it does not affect motor function in sham mice. It also delays spinal cord inflammation resolution in the same mice.. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Soluble: = 10 mg/ml.