ChemicalBook CAS DataBase List 1309444-75-4

1309444-75-4

Name	K145
CAS	1309444-75-4
Molecular Formula	C18H24N2O3S
MDL Number	MFCD28167726
Molecular Weight	348.46
MOL File	1309444-75-4.mol

Chemical Properties

storage temp.	2-8°C
solubility	Soluble in DMSO
form	Powder
color	off-white

Safety Data

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

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

< td class="col2"> U937 cells td>

Cell Line:
Concentration:	0 μM, 4 μM, 6 μM , 8 μM, 10 μM
Incubation Time:	24 hours, 48 hours, 72 hours
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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