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HomeProduct name listK145

K145

K145 Structural

What is K145?

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.

Properties of K145

solubility  Soluble in DMSO
form  Powder

Safety information for K145

Computed Descriptors for K145

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