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M-110 is a novel and highly selective inhibitor of PIM kinases; inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 uM, with no activity on normal human peripheral blood mononuclear cells up to 40 uM.IC50 value:Target: Pim inhibitorin vitro: Treatment of DU-145 cells with M-110 or with a structurally unrelated PIM inhibitor, SGI-1776, significantly reduces pSTAT3Tyr705 expression without affecting the expression of STAT3. Furthermore, treatment of DU-145 cells with M-110 attenuates the interleukin-6-induced increase in pSTAT3Tyr705 [1]. M-110 treatment of APC-mutant DLD-1 cells, preferentially attenuated constitutive TOPFLASH activity as compared with FOPFLASH, and had no effect on the CMV-β-galactosidase control reporter. In SW480 cells, M-110 also decreased the levels of free cytoplasmic β-catenin as determined by E-cadherin pull down assays. M-110 also blocked Wnt signaling when other destruction complex components were disrupted, including abrogation of AXIN1/2 expression using siRNAs or inhibition of GSK3β activity using LiCl or I3M [2].

[1]. He Y, et al. Schisantherin A suppresses osteoclast formation and wear particle-induced osteolysis via modulating RANKL signaling pathways. Biochem Biophys Res Commun. 2014 Jul 4;449(3):344-50. [2]. Zhou E, et al. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Int Immunopharmacol. 2014 Sep;22(1):133-40. [3]. Sa F, et al. Discovery of novel anti-parkinsonian effect of schisantherin A in in vitro and in vivo. Neurosci Lett. 2015 Apr 23;593:7-12. [4]. Zhang LQ, et al. Schisantherin A protects against 6-OHDA-induced dopaminergic neuron damage in zebrafish and cytotoxicity in SH-SY5Y cells through the ROS/NO and AKT/GSK3β pathways. J Ethnopharmacol. 2015 Apr 29. pii: S0378-8741(15)00306-2.
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