HI5 是一种有效的微管蛋白 (tublin)和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]. |
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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. |
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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. |
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| 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. |
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