| Description | M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM. |
| In vitro | M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM. M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50 values of 0.6 to 0.8 μM. M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells (IC50: 0.9 μM). M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation[1]. |
| molecular weight | 445.94 |
| Molecular formula | C22H28ClN5O3 |
| CAS | 1395048-49-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (112.12 mM), Sonication is recommended. |
| References | 1. Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol Cancer Ther. 2010 Sep;9(9):2478-87. 2. 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. 3. 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. 4. 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. 5. 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. |