您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > HI5
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
HI5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HI5图片
CAS NO:2411548-90-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HI5 是一种有效的微管蛋白 (tublin)IDO抑制剂,对 HeLa 细胞的IC50为 70 nM。HI5 抑制 IDO 的表达,减少犬尿氨酸的产生,从而刺激 T 细胞活化和增殖。HI5 对 HeLa 细胞可抑制微管蛋白聚合和细胞迁移,引起 G2/M 期阻滞,同时通过线粒体依赖性凋亡途径诱导细胞凋亡 (apoptosis) 并引起反应性氧化应激。HI5 可用于抗癌研究。
生物活性

HI5 is a potenttublinandIDOinhibitor, with anIC50value of 70 nM in HeLa cells. HI5 inhibitIDOexpression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induceapoptosisvia the mitochondrial dependentapoptosispathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer[1].

IC50& Target

IC50: 70 nM in HeLa[1]

体外研究
(In Vitro)

HI5 (0-10 μM; 72 hours) exhibits potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC[1].
HI5 (0.1 and 0.5 μM; 24 hours) exhibits markedly disruption of microtubule organization in a concentration-dependent manner[1].
HI5 (0.5 μM; 24 hours) significantly up-regulates the expression level of Bax protein, while down-regulates the protein of Bcl-2, furthermore, markedly up-regulates the protein expressions of caspase-3 and PARP[1].

Cell Proliferation Assay

Cell Line:HeLa, PC-3, A549 and HUVEC[1]
Concentration:0-10 μM
Incubation Time:72 hours
Result:Exhibited potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC with IC50s of 0.07 ± 0.005 μM, 0.46 ± 0.06 μM, 0.22 ± 0.10 μM, 1.52 ± 0.09 μM, respectively.

Immunofluorescence

Cell Line:HeLa[1]
Concentration:0.1 and 0.5 μM
Incubation Time:24 hours
Result:Exhibited markedly disruption of microtubule organization in a concentration-dependent manner.

Western Blot Analysis

Cell Line:HeLa[1]
Concentration:0.5 μM
Incubation Time:24 hours
Result:Significantly up-regulated the expression level of Bax protein, while down-regulated the protein of Bcl-2, furthermore, markedly up-regulated the protein expressions of caspase-3 and PARP.
体内研究
(In Vivo)

HI5 (15 and 30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth at a dose-dependent manner[1].

Animal Model:BALB/c nude mice (18-22 g, 5 week-old, injected with HeLa cells)[1]
Dosage:15 and 30 mg/kg
Administration:IV; daily, for 21 days
Result:Significantly inhibited tumor growth at a dose-dependent manner with inhibitory rates of 50.73% and 65.76% at doses of 15 and 30 mg/kg, respectively.
分子量

745.82

Formula

C42H43N5O8

CAS 号

2411548-90-6

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.