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.
For research use only. We do not sell to patients.
- Formula: C30H40N6O6S2
- Molecular Weight:644.81
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Caspase Isoforms
More
Biological Activity
|
Caspase-3 |
Caspase-7 |
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.
-
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 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 %).
-
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.
-
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.
-
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.
Chemical Information
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin/LSD1-IN-1 Related Classifications
HY-176283 Related Classifications
Powered by Bioz