2. Cell Cycle/DNA Damage Cytoskeleton Epigenetics Apoptosis
  3. Microtubule/Tubulin Histone Demethylase Apoptosis Wee1 Bcl-2 Family Caspase
  4. Tubulin/LSD1-IN-1

Tubulin/LSD1-IN-1 是一种有效的微管蛋白聚合和 LSD1 (IC50 = 1.72 μM) 双重抑制剂。Tubulin/LSD1-IN-1 对癌细胞系有广谱抗增殖活性。Tubulin/LSD1-IN-1 通过靶向秋水仙碱结合位点抑制微管蛋白聚合，从而破坏胃癌细胞中的微管网络。Tubulin/LSD1-IN-1 可提高 H3K4me1/2 和 H3K9me2/3 的甲基化水平，从而实现表观遗传调控。Tubulin/LSD1-IN-1 诱导 G2/M 期阻滞、促进细胞凋亡 (Apoptosis)，有效地抑制胃癌细胞的集落形成。

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Tubulin/LSD1-IN-1 Chemical Structure

Tubulin/LSD1-IN-1 Chemical Structure

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Tubulin/LSD1-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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PKMYT1

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells[1].

IC50 & Target

Caspase-3

 

Caspase-7

 

体外研究
(In Vitro)

Tubulin/LSD1-IN-1 (Compound L-6) (10-60 nM, 12-48 h) 对 MGC-803 和 HGC-27 细胞具有剂量和时间依赖性抑制作用，能抑制胃癌细胞的长期增殖能力，对 GES-1 细胞的毒性较低[1]。

Tubulin/LSD1-IN-1 (48 h) 对多种癌细胞的 IC50 均小于100 nM (IC50: MGC-803 = 33 nM, HGC-27 = 49 nM, HTC-116 = 38 nM, KYSE-450 = 48 nM)[1]。

Tubulin/LSD1-IN-1 (10-60 nM, 24-48 h) 在 MGC-803 和 HGC-27 细胞中通过调节细胞周期，抑制微管聚合，阻滞细胞于 G2/M 期[1]。

Tubulin/LSD1-IN-1 (20-60 nM, 48 h) 诱导 MGC-803 和 HGC-27 细胞发生显著的形态变化并凋亡[1]。

Tubulin/LSD1-IN-1 (10-60 nM, 48 h) 可有效抑制 MGC-803 和 HGC-27 细胞中 H3K4me1/2 和 H3K9me2/3 的去甲基化[1]。

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

Tubulin/LSD1-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: MGC-803 cells, HGC-27 cells, GES-1 cells
Concentration: 10 nM, 20 nM, 30 nM, 40 nM, 60 nM
Incubation Time: 12 h, 24 h, 36 h, 48 h
Result: Gradually inhibited cell viability to less than 50% at 48 hours in MGC-803 and HGC-27 cells. Had an IC50 of 300 nM for GES-1 cells.

Cell Cycle Analysis[1]

Cell Line: MGC-803 cells, HGC-27 cells
Concentration: 10 nM, 20 nM, 30 nM, 40 nM, 60 nM
Incubation Time: 24 h
Result: Increased significantly the proportion of cells in the G2/M phase (MGC-803: increased from 26.04 % to 66.88 %; HGC-27: increased from 43.77 % to 56.23 %).

Apoptosis Analysis[1]

Cell Line: MGC-803 cells, HGC-27 cells
Concentration: 20 nM, 30 nM, 40 nM, 60 nM
Incubation Time: 48 h
Result: Caused cell size reduction, nuclear fragmentation, and increased cell death.
Showed apoptotic rates of cells treated with 40 nM and 60 nM as 73.0 % (MGC-803 cells) and 42.66 % (HGC-27 cells), respectively.

Immunofluorescence[1]

Cell Line: MGC-803 cells, HGC-27 cells
Concentration: 20 nM, 30 nM, 40 nM, 60 nM
Incubation Time: 24 h
Result: Caused the microtubule network to fragment and accumulate in the perinuclear region, consistent with the action of colchicine.

Western Blot Analysis[1]

Cell Line: MGC-803 cells, HGC-27 cells
Concentration: 10 nM, 20 nM, 30 nM, 40 nM, 60 nM
Incubation Time: 48 h
Result: Downregulated Cyclin A1/2, Cyclin B1, p-CDC2 (Thr14/161), and Wee1 among the cell cycle-related proteins; and upregulated p-Histone H3.
Upregulated cleaved Caspase-3/7 and cleaved PARP among apoptosis-related proteins; downregulated Bcl-2.
分子量

644.81

Formula

C30H40N6O6S2
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

Tubulin/LSD1-IN-1 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:

Tubulin/LSD1-IN-1Microtubule/TubulinHistone DemethylaseApoptosisWee1Bcl-2 FamilyCaspaseTubulinLSD1MGC-803 cellsHGC-27 cellsAntiproliferativeGastric cancerInhibitorinhibitorinhibit

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