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MN58b

  Cat. No.:  DC21335   Featured
Chemical Structure
203192-01-2
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More than 5000 active chemicals with high quality for research!
Field of application
MN58b is a potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.4 uM, >30-fold selectivity over ChoKβ and does not affect MAPKs, PI3Ks, and other enzymes involved in the regulation of phospholipid metabolism.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 203192-01-2
Chemical Name: 1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide
Synonyms: MN-58b;MN 58b
SMILES: C(C1=CC=C(C[NH0+]2C=CC(N(C)C)=CC=2)C=C1)CCCC1=CC=C(C[NH0+]2C=CC(N(C)C)=CC=2)C=C1.[BrH0-].[BrH0-]
Formula: C32H40Br2N4
M.Wt: 640.508
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].
Target: Choline kinase α (CHKα)[1]
In Vivo: 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[2]. Animal Model: MF-1 nude mice with HT29 or MDA-MB-231 cells[2] Dosage: 4 mg/kg Administration: Intraperitoneal injection; once a day; for 5 days Result: Phosphomonoesters decreased significantly.
In Vitro: The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively[1]. 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[1]. 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[1]. Cell Viability Assay[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 5 µM Incubation Time: 72 hours Result: Inhibited cells growth. Apoptosis Analysis[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 2 µM, 5 µM, 10 µM Incubation Time: 24 and 48 hours Result: Induced cell apoptosis.
References: [1]. Mazarico JM, et al. Choline Kinase Alpha (CHKα) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors. Mol Cancer Ther. 2016 Feb;15(2):323-33. [2]. Al-Saffar NM, et al. 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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