1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Kinesin

Dimethylenastron 

Cat. No.: HY-19944 Purity: 98.12%
Handling Instructions

Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.

For research use only. We do not sell to patients.

Dimethylenastron Chemical Structure

Dimethylenastron Chemical Structure

CAS No. : 863774-58-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.

IC50 & Target[1]

Eg5

200 nM (IC50)

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[1]. 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[2].

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[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (102.52 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3070 mL 16.5349 mL 33.0699 mL
5 mM 0.6614 mL 3.3070 mL 6.6140 mL
10 mM 0.3307 mL 1.6535 mL 3.3070 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Cell invasion in response to Dimethylenastron is carried out by transwell assays. The upper surface of the transwell filters is coated with matrigel or fibronectin. Cells suspended in 200 μL serum-free media are added to the chamber, and the chamber is placed in a 24-well plate containing complete medium. After 24 h of incubation at 37°C, the filters are gently taken out and matrigel on the upper surface of the filters is removed by cotton swabs. Cells on the underside of transwell filters are fixed with 4% paraformaldehyde for 30 min, stained with 0.1% crystal violet for 10 min, and then photographed. For quantitative assessment, the number of invading cells is counted in five random fields per filter. The extent of cell invasion is quantified as the number of invading cells in the drug-treatment group divided by the number of invading cells in the control group[2].

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

Animal Administration
[3]

Just after the conjunctival suture is closed, a metallic needle (30 G) is inserted into the subconjunctival space at the nasal margin of the superior rectus muscle and injection of one of the following agents is delivered: The rabbits receive either no adjuvant after the surgery in the control group, one unilateral subconjunctival injection of Dimethylenastron (1.0 µmol, 3.0 µmol) or of the vehicle (DMSO, 99.9%, 10 mg/mL) alone at baseline, which means an injection directly after surgery and in two further groups additionally at days 3 and 7 thereafter (1.0 µmol, 3.0 µmol)[3].

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

References
Molecular Weight

302.39

Formula

C₁₆H₁₈N₂O₂S

CAS No.

863774-58-7

SMILES

O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Dimethylenastron
Cat. No.:
HY-19944
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Dimethylenastron

Cat. No.: HY-19944