3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐
中文名称:
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐
中文同义词:
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐;SPHK2抑制剂(K145盐酸盐)
英文名称:
K145 (hydrochloride)
英文同义词:
SphK2 inhibitor;SPHK2 INHIBITOR;K 145 HYDROCHLORIDE;K-145 HYDROCHLORIDE;K145 (hydrochloride);K145(HCl);3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione hydrochloride (1:1);3-(2-Amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione hydrochloride;K14 (hydrochloride);K145 hydrochloride >=98% (HPLC)
CAS号:
1449240-68-9
分子式:
C18H25ClN2O3S
分子量:
384.9207
EINECS号:
相关类别:
细胞生物学试剂;API
Mol文件:
1449240-68-9.mol
储存条件
2-8°C
溶解度
DMSO: soluble20mg/mL, clear
形态
powder
颜色
white to beige
生物活性
K145 hydrochloride 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 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡，并具有强大的抗肿瘤活性。
靶点
IC50: 4.3 µM (SphK2)
Ki: 6.4 µM (SphK2)
体外研究
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: 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
Cell Line: U937 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Significantly induced apoptosis in U937 cells.
Western Blot Analysis
Cell Line: U937 cells
Concentration: 4 µM, 8 µM
Incubation Time: 3 hours
Result: Phosphorylated ERK and Akt were decreased.
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.
Cell Line:
U937 cells
Concentration:
10 µM
Incubation Time:
24 hours
Result:
Significantly induced apoptosis in U937 cells.
Cell Line:
U937 cells
Concentration:
4 µM, 8 µM
Incubation Time:
3 hours
Result:
Phosphorylated ERK and Akt were decreased.
体内研究
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: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
Animal Model:
BALB/c-nu mice injected with U937 cells
Dosage:
50 mg/kg
Administration:
Oral gavage; daily; for 15 days
Result:
Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
WGK Germany
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