Dimethylenastron

SKU: orb1223823

Description

A small molecule inhibitor of the mitotic kinesin Eg5; inhibits endothelial cell proliferation and migration in vitro; exhibits a shorter mitotic arrest, bipolar or multipolar karyokinesis, followed by apoptosis of the daughter cells in dimethylenastron-treated tetraploid cells.

Key Properties

• CAS Number: 863774-58-7
• MW: 302.3913
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₈N₂O₂S
• SMILES: O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1
• Target: Kinesin
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vivo:
  Dimethylenastron (1.0 μmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0 μmol) reveals a markedly reduced ratio of intraocular pressure and a milder, but not obviously reduced, subconjunctival fibrotic reaction in the rabbits treated with glaucoma filtration surgery.
• In Vitro:
  Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM. Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells. Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dimethylenastron

Quick Database Links

Gene Symbol

Kinesin