2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. 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。

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IDO/Tubulin-IN-2

IDO/Tubulin-IN-2 Chemical Structure

CAS No. : 2409479-24-7

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IDO/Tubulin-IN-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

IC50 & Target

TDO, Tubulin[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.041 μM
Compound: HT2
Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
[PMID: 31830637]
HCT-116 IC50
0.095 μM
Compound: HT2
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
[PMID: 31830637]
HepG2 IC50
0.036 μM
Compound: HT2
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
[PMID: 31830637]
L02 IC50
1.04 μM
Compound: HT2
Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
[PMID: 31830637]
U-87MG ATCC IC50
0.43 μM
Compound: HT2
Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
[PMID: 31830637]
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].

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

IDO/Tubulin-IN-2 相关抗体:

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.
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].

MCE 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.
分子量

860.87

Formula

C48H40N6O10
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

IDO/Tubulin-IN-2 相关分类

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  • 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.

Keywords:

IDO/Tubulin-IN-22409479-24-7Microtubule/TubulinApoptosisAntitumorHepG2A549 cellsLow toxicityICR miceBALB/c nude miceInhibitorinhibitorinhibit

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