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K145 hydrochloride

CAS# 1449240-68-9

K145 hydrochloride

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K145 hydrochloride

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Chemical Properties of K145 hydrochloride

Cas No. 1449240-68-9 SDF Download SDF
PubChem ID 76849910 Appearance Powder
Formula C18H25ClN2O3S M.Wt 384.92
Type of Compound N/A Storage Desiccate at -20°C
Synonyms SphK2 inhibitor
Solubility H2O : 126.7 mg/mL (329.16 mM; Need ultrasonic and warming)
DMSO : 50 mg/mL (129.90 mM; Need ultrasonic)
Chemical Name (5Z)-3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-1,3-thiazolidine-2,4-dione;hydrochloride
SMILES CCCCOC1=CC=C(C=C1)CCC=C2C(=O)N(C(=O)S2)CCN.Cl
Standard InChIKey HADFDMGQKBGVAV-NKBLJONXSA-N
Standard InChI InChI=1S/C18H24N2O3S.ClH/c1-2-3-13-23-15-9-7-14(8-10-15)5-4-6-16-17(21)20(12-11-19)18(22)24-16;/h6-10H,2-5,11-13,19H2,1H3;1H/b16-6-;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of K145 hydrochloride

DescriptionK145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM. IC50 value: 4.3 uM [1] Target: SphK2 in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). 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 [1]. in vivo: 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].

References:
[1]. Liu K, et al. 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. PLoS One. 2013;8(2):e56471.

K145 hydrochloride Dilution Calculator

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K145 hydrochloride Molarity Calculator

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Preparing Stock Solutions of K145 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5979 mL 12.9897 mL 25.9794 mL 51.9588 mL 64.9486 mL
5 mM 0.5196 mL 2.5979 mL 5.1959 mL 10.3918 mL 12.9897 mL
10 mM 0.2598 mL 1.299 mL 2.5979 mL 5.1959 mL 6.4949 mL
50 mM 0.052 mL 0.2598 mL 0.5196 mL 1.0392 mL 1.299 mL
100 mM 0.026 mL 0.1299 mL 0.2598 mL 0.5196 mL 0.6495 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on K145 hydrochloride

K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.

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Description

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.

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