1. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  2. Microtubule/Tubulin Indoleamine 2,3-Dioxygenase (IDO) Apoptosis
  3. HI5

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。

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HI5 Chemical Structure

HI5 Chemical Structure

CAS No. : 2411548-90-6

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查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression 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 induce apoptosis via the mitochondrial dependent apoptosis pathway 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HI5
目录号:
HY-146261
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