K145 - CAS 1309444-75-4
Catalog number:
1309444-75-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H24N2O3S
Molecular Weight:
348.46
COA:
Inquire
Targets:
SPHK
Description:
K145 is a selective sphingosine kinase-2 (SphK2) inhibitor and anticancer agent. K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 µM. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells. K145 exhibits comparable in vivo anti-tumor activity to tamibarotene, while concomitantly exhibiting less toxicity in this U937 xenograft cancer model.
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Purity:
>98%
Synonyms:
SphK2 inhibitor; K 145; K-145
MSDS:
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1.Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent.
Liu K1, Guo TL, Hait NC, Allegood J, Parikh HI, Xu W, Kellogg GE, Grant S, Spiegel S, Zhang S. PLoS One. 2013;8(2):e56471. doi: 10.1371/journal.pone.0056471. Epub 2013 Feb 20.
In our effort to develop selective sphingosine kinase-2 (SphK2) inhibitors as pharmacological tools, a thiazolidine-2,4-dione analogue, 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145), was synthesized and biologically characterized. Biochemical assay results indicate that K145 is a selective SphK2 inhibitor. Molecular modeling studies also support this notion. In vitro studies using human leukemia U937 cells demonstrated that K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways. K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent.
2.Interactions of acetylcholine binding site residues contributing to nicotinic acetylcholine receptor gating: role of residues Y93, Y190, K145 and D200.
Mallipeddi PL1, Pedersen SE, Briggs JM. J Mol Graph Model. 2013 Jul;44:145-54. doi: 10.1016/j.jmgm.2013.05.010. Epub 2013 Jun 15.
The nicotinic acetylcholine receptor exhibits multiple conformational states, resting (channel closed), active (channel open) and desensitized (channel closed). The resting state may be distinguished from the active and desensitized states by the orientation of loop C in the extracellular ligand binding domain (LBD). Homology modeling was used to generate structures of the Torpedo californica α2βδγ nAChR that initially represent the resting state (loop C open) and the desensitized state (loop C closed). Molecular dynamics (MD) simulations were performed on the extracellular LBD on each nAChR conformational state, with and without the agonist anabaseine present in each binding site (the αγ and the αδ sites). Three MD simulations of 10ns each were performed for each of the four conditions. Comparison of dynamics revealed that in the presence of agonist, loop C was drawn inward and attains a more stable conformation. Examination of side-chain interactions revealed that residue αY190 exhibited hydrogen-bonding interactions either with residue αY93 in the ligand binding site or with residue αK145 proximal to the binding site.
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CAS 1309444-75-4 K145

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