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 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.

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Tubulin/LSD1-IN-1 Chemical Structure

Tubulin/LSD1-IN-1 Chemical Structure

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Tubulin/LSD1-IN-1 Related Antibodies

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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

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Description

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

 

In Vitro

Tubulin/LSD1-IN-1 (Compound L-6) (10-60 nM, 12-48 h) has a dose- and time-dependent inhibitory effect on MGC-803 and HGC-27 cells, inhibits the long-term proliferation of gastric cancer cells, and has low toxicity to GES-1 cells[1].

Tubulin/LSD1-IN-1 (48 h) has an IC50 of less than 100 nM against various cancer cells (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) regulates the cell cycle in MGC-803 and HGC-27 cells, inhibits microtubule polymerization, and arrests cells in the G2/M phase[1].

Tubulin/LSD1-IN-1 (20-60 nM, 48 h) induces significant morphological changes and apoptosis in MGC-803 and HGC-27 cells[1].

Tubulin/LSD1-IN-1 (10-60 nM, 48 h) can effectively suppresses the deme thylation of the H3K4me1/2 and H3K9me2/3 in MGC-803 and HGC-27 cells[1].

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

Tubulin/LSD1-IN-1 Related Antibodies

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.
Molecular Weight

644.81

Formula

C30H40N6O6S2
SMILES

S=C(N1CCN(C(C)C)CC1)SCC2=CN(CC(N(CC3=CC=C(OC)C(O)=C3)C4=CC(OC)=C(OC)C(OC)=C4)=O)N=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tubulin/LSD1-IN-1 Related Classifications

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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.

Keywords:

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

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