1. Apoptosis
  2. Apoptosis
  3. TACC3 inhibitor 1

TACC3 inhibitor 1 是一种有效的,可透过血脑屏障的 TACC3 抑制剂。TACC3 inhibitor 1 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G2/M 期。TACC3 inhibitor 1 诱导细胞内 ROS 的产生。TACC3 inhibitor 1 具有抗增殖和抗肿瘤活性。

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TACC3 inhibitor 1

TACC3 inhibitor 1 Chemical Structure

CAS No. : 3033646-06-6

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  • 生物活性

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生物活性

TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
JIMT-1 IC50
4.84 μM
Compound: 7g
Antiproliferative activity against human JIMT-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human JIMT-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332551]
MDA-MB-231 IC50
6.46 μM
Compound: 7g
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332551]
SK-OV-3 IC50
8.21 μM
Compound: 7g
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332551]
U-251 IC50
5.61 μM
Compound: 7g
Cytotoxicity against human U251 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human U251 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 36332551]
U-87MG ATCC IC50
27.54 μM
Compound: 7g
Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 36332551]
U-87MG ATCC IC50
3.29 μM
Compound: 7g
Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36332551]
体外研究
(In Vitro)

TACC3 inhibitor 1 (compound 7g) (1, 2, 4 µM; 36 h) 诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]
TACC3 inhibitor 1 (1, 2, 4 µM; 36 h) 降低线粒体膜电位并诱导细胞内 ROS 的产生[1]
TACC3 inhibitor 1 (1, 2, 4 µM; 24 h) 抑制 U87 细胞的迁移和侵袭[1]

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

Cell Proliferation Assay[1]

Cell Line: U251, U87, MDA-MB-231, JIMT-1, SKOV-3, HLF-1 cells
Concentration: 0-100 µM
Incubation Time: 24 h
Result: Showed antiproliferative activities with IC50s of 5.61, 3.29, 6.46, 4.84, 8.21, 23.11 µM for U251, U87, MDA-MB-231, JIMT-1, SKOV-3, HLF-1 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: U87 cells
Concentration: 1, 2, 4 µM
Incubation Time: 36 h
Result: Induced cell cycle arrest at G2/M phase with the 41.2% cells at G2/M phase at 4 µM.

Apoptosis Analysis[1]

Cell Line: U87 cells
Concentration: 1, 2, 4 µM
Incubation Time: 36 h
Result: Induced apoptosis in a dose-dependent manner with the percentage of early apoptotic cells increased from 4.49% in control group to 21.42%, late apoptotic cells increased from 0.52% to 26.72% at 4 µM.
体内研究
(In Vivo)

TACC3 inhibitor 1 (20 mg/kg; i.p.; daily for 20 days) 在小鼠体内显示出抗肿瘤活性[1]

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

Animal Model: Six-week-old BALB/c nude mice (U87 xenograft model)[1]
Dosage: 20 mg/kg
Administration: I.p.; daily for 20 days
Result: Exhibited a significant tumor growth regression and no observable toxicity during the administration period and had no effects on the body weight.
分子量

379.48

Formula

C20H21N5OS

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
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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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TACC3 inhibitor 1
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HY-151985
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