M-110

• CAT Number: I001515
• CAS Number: 1395048-49-3
• Molecular Formula: C22H28ClN5O3
• Molecular Weight: 445.94
• Purity: ≥95%
• Synonyms: N-[(E)-1-(4-chloro-2-hydroxyphenyl)propylideneamino]-2-(3-morpholin-4-ylpropylamino)pyridine-4-carboxamide
• InChI: InChI=1S/C22H28ClN5O3/c1-2-19(18-5-4-17(23)15-20(18)29)26-27-22(30)16-6-8-25-21(14-16)24-7-3-9-28-10-12-31-13-11-28/h4-6,8,14-15,29H,2-3,7,9-13H2,1H3,(H,24,25)(H,27,30)/b26-19+
• InChIKey: FXXCNYVQIONABS-LGUFXXKBSA-N
• SMILES: CCC(=NNC(=O)C1=CC(=NC=C1)NCCCN2CCOCC2)C3=C(C=C(C=C3)Cl)O

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[1].
M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM[1]. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM[1].
M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation[1].
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[1].

Reference

[1]. Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol Cancer Ther. 2010 Sep;9(9):2478-87.
 [Content Brief]

[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.
 [Content Brief]

[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.
 [Content Brief]

[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.
 [Content Brief]

[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.
 [Content Brief]