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Eg5 Inhibitor III(Dimethylenastron)

  Cat. No.:  DC9270   Featured
Chemical Structure
863774-58-7
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Field of application
Eg5 Inhibitor III, Dimethylenastron is a cell-permeable quinazoline-thione compound that acts as a strong, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5.
Cas No.: 863774-58-7
Chemical Name: Dimethylenastron
Synonyms: 5(1H)-Quinazolinone,2,3,4,6,7,8-hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-;Dimethylenastron;4-(3-hydroxyphenyl)-7,7-dimethyl-2-sulfanylidene-3,4,6,8-tetrahydro-1H-quinazolin-5-one;Dimethylnasetron;Eg5 Inhibitor III, Dimethylenastron;Rac-Dimethylenastron;2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone;7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione;Eg5 inhibitor III;AOB2736;SYN5065;BCP17179;AK548019;Eg5 Inhib
SMILES: S=C1N([H])C([H])(C2C([H])=C([H])C([H])=C(C=2[H])O[H])C2C(C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C=2N1[H])=O
Formula: C16H18N2O2S
M.Wt: 302.3913
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC5137 SB 743921 SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.
DC2082 Monastrol Monastrol is a reversible, cell-permeable inhibitor of the motor protein Eg5 (kinesin family protein 11, Kif11), blocking basal ATPase activity in vitro (IC50 = 6.1 µM) and inducing the formation of monoastral spindles in cell-based assays (IC50 = 51.3 μM
DC9272 K 858 K 858 is an ATP-uncompetitive mitotic kinesin Eg5 inhibitor, which does not effect microtubule dynamics.
DC5107 SB-715992 (Ispinesib) Ispinesib (SB 715992) is a potent mitotic kinesin KSP (Eg5) inhibitor with a Ki and an IC50 of 0.6 and 4.1 nM, respectively.
DC7812 GSK923295 GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.
DC9270 Eg5 Inhibitor III(Dimethylenastron) Eg5 Inhibitor III, Dimethylenastron is a cell-permeable quinazoline-thione compound that acts as a strong, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5.
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