MN58b is a selective choline kinase α (CHKα) inhibitor. MN58b is a novel anticancer drug that inhibits choline kinase, resulting in inhibition of phosphocholine synthesis. Inhibition of choline kinase by MN58b resulted in altered phospholipid metabolism both in cultured tumor cells and in vivo.
Chemical Formula: C32H40Br2N4
Molecular Weight: 640.508
Elemental Analysis: C, 60.01; H, 6.30; Br, 24.95; N, 8.75
Chemical Name: 1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide
InChi Key: 1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide
InChi Code: InChI=1S/C32H40N4.2BrH/c1-33(2)31-17-21-35(22-18-31)25-29-13-9-27(10-14-29)7-5-6-8-28-11-15-30(16-12-28)26-36-23-19-32(20-24-36)34(3)4;;/h9-24H,5-8,25-26H2,1-4H3;2*1H/q+2;;/p-2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively.
MN58b (1-5 µM; 72 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) has a marked effect on colony formation at 1 µM, and growth is completely abolished at 5 µM in all the cell lines.
MN58b ((1-10 µM; 24-48 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) induces apoptosis and this response correlates with CHKα expression.
MN58b (4 mg/kg; intraperitoneal injection; once a day; for 5 days; MF-1 nude mice) treatment significantly decreases phosphomonoesters in both HT29 and MDA-MB-231 xenografts. Phosphocholine levels are found to correlate with choline kinase activities.
Al-Saffar NM, Troy H, Ramírez de Molina A, Jackson LE, Madhu B, Griffiths JR, Leach MO, Workman P, Lacal JC, Judson IR, Chung YL. Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res. 2006 Jan 1;66(1):427-34. doi: 10.1158/0008-5472.CAN-05-1338. PMID: 16397258.
Li Y, Kinting S, Höppner S, Forstner ME, Uhl O, Koletzko B, Griese M. Metabolic labelling of choline phospholipids probes ABCA3 transport in lamellar bodies. Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Dec;1864(12):158516. doi: 10.1016/j.bbalip.2019.158516. Epub 2019 Aug 29. PMID: 31473345.
Kumar M, Arlauckas SP, Saksena S, Verma G, Ittyerah R, Pickup S, Popov AV, Delikatny EJ, Poptani H. Magnetic resonance spectroscopy for detection of choline kinase inhibition in the treatment of brain tumors. Mol Cancer Ther. 2015 Apr;14(4):899-908. doi: 10.1158/1535-7163.MCT-14-0775. Epub 2015 Feb 5. PMID: 25657334; PMCID: PMC4394035.
Guma M, Sanchez-Lopez E, Lodi A, Garcia-Carbonell R, Tiziani S, Karin M, Lacal JC, Firestein GS. Choline kinase inhibition in rheumatoid arthritis. Ann Rheum Dis. 2015 Jul;74(7):1399-407. doi: 10.1136/annrheumdis-2014-205696. Epub 2014 Oct 1. PMID: 25274633; PMCID: PMC4382461.
Zimmerman T, Moneriz C, Diez A, Bautista JM, Gómez Del Pulgar T, Cebrián A, Lacal JC. Antiplasmodial activity and mechanism of action of RSM-932A, a promising synergistic inhibitor of Plasmodium falciparum choline kinase. Antimicrob Agents Chemother. 2013 Dec;57(12):5878-88. doi: 10.1128/AAC.00920-13. Epub 2013 Sep 16. PMID: 24041883; PMCID: PMC3837925.
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