K145
Based on 6 publication(s) in Google Scholar
K145 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 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
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- CAS. Nr.: 1309444-75-4
- Formel: C18H24N2O3S
- Molecular Weight:348.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) K145
More- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Channels. 2020 Dec;14(1):216-230. [Abstract]
- Exp Mol Pathol. 2016 Feb;100(1):51-8. [Abstract]
- Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]
- Biochem Biophys Res Commun. 2021 Sep 28;580:1-6. [Abstract]
- Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. [Abstract]
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Biologische Aktivität
K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 cells
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Concentration:0 µM, 4 µM, 6 µM, 8 µM, 10 µM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Significantly inhibited the growth of U937 cells in a concentration-dependent manner.
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Cell Line:U937 cells
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Concentration:10 µM
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Incubation Time:24 hours
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Result:Significantly induced apoptosis in U937 cells.
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Cell Line:U937 cells
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Concentration:4 µM, 8 µM
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Incubation Time:3 hours
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Result:Phosphorylated ERK and Akt were decreased.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu mice injected with U937 cells[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; daily; for 15 days
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Result:Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
Chemical Information
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CAS. Nr. 1309444-75-4
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Molecular Weight 348.46
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Formel C18H24N2O3S
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SMILES
O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Channels
Sphingosine kinase 2 inhibitor ABC294640 suppresses neuronal excitability and inhibits multiple endogenously and exogenously expressed voltage-gated ion channels in cultured cells. [Abstract]2020 Dec;14(1):216-230. PMID: 32615066 -
Exp Mol Pathol
Hypoxic preconditioning protects cardiomyocytes against hypoxia/reoxygenation-induced cell apoptosis via sphingosine kinase 2 and FAK/AKT pathway. [Abstract]2016 Feb;100(1):51-8. PMID: 26621495 -
Am J Cancer Res
Targeting sphingosine kinase 2 suppresses cell growth and synergizes with BCL2/BCL-XL inhibitors through NOXA-mediated MCL1 degradation in cholangiocarcinoma. [Abstract]2019 Mar 1;9(3):546-561. PMID: 30949409
K145 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]
Western immunoblotting analysis of NOXA protein levels in RBE and HCCC9810 cells treated with different concentrations of K145 for 24 h. Data shown represents 2 independent experiments.
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Biochem Biophys Res Commun
The alleviating effect of sphingosine kinases 2 inhibitor K145 on nonalcoholic fatty liver. [Abstract]2021 Sep 28;580:1-6. PMID: 34607257 -
Biochem Biophys Res Commun
3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) ameliorated dexamethasone induced hepatic gluconeogenesis through activation of Akt/FoxO1 pathway. [Abstract]2017 Nov 4;493(1):286-290. PMID: 28911865
K145 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. [Abstract]
Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.
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