K145 是一种选择性的，具有底物竞争性和口服活性的SphK2抑制剂，IC50为 4.3 μM，Ki为 6.4 μM。K145 对 SphK1 和其他蛋白激酶没有活性。K145 可诱导细胞凋亡，并具有强大的抗肿瘤活性。
| 生物活性 | K145 is a selective, substrate-competitive and orally activeSphK2inhibitor with anIC50of 4.3 μM and aKiof 6.4 μM. K145 is inactive againstSphK1and other protein kinases. K145 induces cellapoptosisand has potently antitumor activity[1]. |
| IC50& Target | IC50: 4.3 μM (SphK2)[1]
Ki: 6.4 μM (SphK2)[1] |
体外研究
(In Vitro) | 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].
Cell Viability Assay[1] | Cell Line: | U937 cells | | 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[1] | Cell Line: | U937 cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Significantly induced apoptosis in U937 cells. |
Western Blot Analysis[1] | Cell Line: | U937 cells | | Concentration: | 4 μM, 8 μM | | Incubation Time: | 3 hours | | Result: | Phosphorylated ERK and Akt were decreased. |
|
体内研究
(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[1].
| Animal Model: | BALB/c-nu mice injected with U937 cells[1] | | 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. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
