| Identification | Back Directory | [Name]
2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide | [CAS]
1395048-49-3 | [Synonyms]
M-110
CS-2124
M-110 >=98% (HPLC)
2-[[3-(4-Morpholinyl)propyl]amino]-4-pyridinecarboxylic acid 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide
4-Pyridinecarboxylic acid, 2-[[3-(4-morpholinyl)propyl]amino]-, 2-[1-(4-chloro-2-hydroxyphenyl)propylidene]hydrazide | [Molecular Formula]
C22H28ClN5O3 | [MOL File]
1395048-49-3.mol | [Molecular Weight]
445.94 |
| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble25mg/mL, clear | [form ]
powder | [pka]
7.46±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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]. | [Biochem/physiol Actions]
M-110 is a highly isoform-selective, cell permeable and potent ATP-competitive inhibitor of the PIM kinase family that prefers PIM-3. M-110 is an inhibitor of Wnt/β-catenin signaling that act downstream of the symb-catenin destruction complex to inhibit both Wnt-induced and cancer associated constitutive Wnt signaling via destabilization of β-catenin. The compound chelates iron in vitro and in intact cells. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM, with no activity on normal human peripheral blood mononuclear cells up to 40 μM. | [storage]
Store at -20°C | [References]
[1] Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol?Cancer?Ther.?2010 Sep;9(9):2478-87. DOI:10.1158/1535-7163.MCT-10-0321
[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. DOI:10.1016/j.bbrc.2014.05.034
[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. DOI:10.1016/j.intimp.2014.06.004
[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. DOI:10.1016/j.neulet.2015.03.016
[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. DOI:10.1016/j.jep.2015.04.040 |
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