Dimethylenastron

Cat. No.: HY-19944 Purity: 98.68%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Dimethylenastron Chemical Structure

CAS No. : 863774-58-7

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Dimethylenastron

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Dimethylenastron is a potent kinesin 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].

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

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].

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

Molecular Weight

302.39

Appearance

Solid

Formula

C₁₆H₁₈N₂O₂S

CAS No.

863774-58-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (330.70 mM; Need ultrasonic)

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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 98.68%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (255 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[1]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7. [Content Brief]

[2]. Sun XD, et al. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8. [Content Brief]

[3]. Lüke J, et al. The effect of adjuvant dimethylenastron, a mitotic Kinesin Eg5 inhibitor, in experimental glaucoma filtration surgery. Curr Eye Res. 2010 Dec;35(12):1090-8. [Content Brief]

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	[1]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7. [Content Brief] [2]. Sun XD, et al. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8. [Content Brief] [3]. Lüke J, et al. The effect of adjuvant dimethylenastron, a mitotic Kinesin Eg5 inhibitor, in experimental glaucoma filtration surgery. Curr Eye Res. 2010 Dec;35(12):1090-8. [Content Brief]