上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
IDO/Tubulin-IN-2
IDO/Tubulin-IN-2 (HT2) 是一种有效的 TDO 和微管蛋白 (tubulin) 抑制剂。IDO/Tubulin-IN-2 对 U87、HepG2、A549、HCT-116 和 LO2 癌细胞具有较强的抗肿瘤活性，其 IC50 分别为 0.43、0.036、0.041、0.095和1.04 μM。IDO/Tubulin-IN-2 显著提高抗肿瘤活性。
IDO/Tubulin-IN-2 Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity[1].
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IC50 & Target |
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体外研究
(In Vitro) |
IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity with IC50 values between 0.036 and 0.43 μM against cancer cell lines[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) has strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3[1].
IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner[1].
IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: |
Human cancer cell lines and non-tumoral cell line[1] |
| Concentration: |
0-50 μM |
| Incubation Time: |
4 h |
| Result: |
Displayed potent cytotoxicity with IC50 values of 0.43 μM (U87), 0.036 μM (HepG2), 0.041 μM (A549), 0.095 μM (HCT-116), and 1.04 μM (LO2). |
Cell Cycle Analysis
| Cell Line: |
HepG2 cells[1] |
| Concentration: |
0.1 μM |
| Incubation Time: |
24 h |
| Result: |
Arrested the HepG2 cells cycle mainly at the G2 phase. |
Apoptosis Analysis
| Cell Line: |
HepG2 cells[1] |
| Concentration: |
0.1 μM |
| Incubation Time: |
24 h |
| Result: |
Effectively caused cell apoptosis, the percentage of apoptosis cells increased to 54% |
Western Blot Analysis
| Cell Line: |
HepG2 cells[1] |
| Concentration: |
0.1 μM |
| Incubation Time: |
24 h |
| Result: |
Showed strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3, which could lead to cell death at last. |
RT-PCR
| Cell Line: |
HepG2 cells[1] |
| Concentration: |
0.05 μM |
| Incubation Time: |
24, 48 and 72 h |
| Result: |
Markedly decreased mRNA expression level of TDO at a time-dependent manner. |
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体内研究
(In Vivo) |
IDO/Tubulin-IN-2 (HT2) (30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth[1].
IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)[1] |
| Dosage: |
30 mg/kg |
| Administration: |
Intravenously injected via a tail vein; daily, for 21 days |
| Result: |
Significantly inhibited tumor growth. |
| Animal Model: |
Male A549 tumor xenograft BALB/c nude mice (5 weeks, 18-22 g)[1] |
| Dosage: |
30 mg/kg |
| Administration: |
IV, daily, for 29 days |
| Result: |
Had effective antitumor immunity ability to promote the tumor therapeutic efficacy. |
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Hua S, Chen F, Gou S. Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase. Eur J Med Chem. 2020;187:111949.
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