Eg5 Inhibitor III

Eg5 Inhibitor III is an inhibitor of mitotic motor kinesin Eg5 (IC50 = 200 nM). Eg5 Inhibitor III suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. The inhibition of kinesin Eg5 by small molecules such as monastrol is currently evaluated as an approach to develop a novel class of antiproliferative drugs for the treatment of malignant tumours.

Product information

CAS Number: 863774-58-7

Molecular Weight: 302.39

Formula: C16H18N2O2S

Synonym:

Dimethylenastron

Eg5Inhibitor III

Eg5Inhibitor  III

Eg5  InhibitorIII

Chemical Name: 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone

Smiles: CC1(C)CC2NC(=S)NC(C=2C(=O)C1)C1C=C(O)C=CC=1

InChiKey: RUOOPLOUUAYNPY-UHFFFAOYSA-N

InChi: InChI=1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Eg5 Inhibitor III is a potent Eg5 inhibitor, with an IC50 of 200 nM. Eg5 Inhibitor III exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Eg5 Inhibitor III (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells. Eg5 Inhibitor III (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. Eg5 Inhibitor III also reduces invasion ability of the cancer cells.

In Vivo:

Eg5 Inhibitor III (1.0 µmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Eg5 Inhibitor III (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.

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.
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.
3. Luke 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.

Products are for research use only. Not for human use.