| Identification | Back Directory | [Name]
K145 | [CAS]
1309444-75-4 | [Synonyms]
K145
3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]- | [Molecular Formula]
C18H24N2O3S | [MDL Number]
MFCD28167726 | [MOL File]
1309444-75-4.mol | [Molecular Weight]
348.46 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with IC50 of 4.3 μM and Ki of 6.4 μM.It is inactive against SphK1 and other protein kinases,it induces apoptosis and has potent antitumor activity. | [in vitro]
K145 (0-10 μM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.
K145 (10 μM; 24 hours; U937 cells) ) treatment significantly induces apoptosis in U937 cells.
K145 (4-8 μM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.
Treatment with K145 (10 μM) causes a decrease of total cellular S1P without significant effects on ceramide levels. Cell Viability Assay | Cell Line: | < td class="col2"> U937 cells | Concentration: | 0 μM, 4 μM, 6 μM , 8 μM, 10 μM | | Incubation Time: | 24 hours, 48 hours, 72 hours | td> | Result: | Significantly inhibited the growth of U937 cells in a concentration-dependent manner. | Apoptosis Analysis | Cell Line: | U937 cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Significantly induced apoptosis in U937 cells. | Western Blot Analysis < /p> | Cell Line: | U937 cells | | Concentration: | 4 μM, 8 μM | | Incubation Time: < /td> | 3 hours | | Result: | Phosphorylated ERK and Akt wer e decreased. | | [in vivo]
K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice. | Animal Model: | BALB/c-nu mice injected with U937 cells | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; daily; for 15 days | | Result: | Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. | | [target]
IC50: 4.3 μM (SphK2)
Ki: 6.4 μM (SphK2) | [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. DOI:10.1371/journal.pone.0056471 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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