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1309444-75-4

中文名稱 1309444-75-4
英文名稱 K145
CAS 1309444-75-4
分子式 C18H24N2O3S
分子量 348.46
MOL 文件 1309444-75-4.mol
1309444-75-4 結(jié)構(gòu)式 1309444-75-4 結(jié)構(gòu)式

基本信息

英文別名
K145
3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

溶解度溶于二甲基亞砜
形態(tài)粉末

常見問(wèn)題列表

生物活性
K145 是一種選擇性的,具有底物競(jìng)爭(zhēng)性和口服活性的 SphK2 抑制劑,IC50 為 4.3 μM,Ki 為 6.4 μM。K145 對(duì) SphK1 和其他蛋白激酶沒(méi)有活性。K145 可誘導(dǎo)細(xì)胞凋亡,并具有強(qiáng)大的抗腫瘤活性。
靶點(diǎn)

IC50: 4.3 μM (SphK2)
Ki: 6.4 μM (SphK2)

體外研究

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.
體內(nèi)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: Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
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