Molecular Formula | C16H18N2O2S |
Molar Mass | 302.39 |
Density | 1.34±0.1 g/cm3(Predicted) |
Boling Point | 475.6±55.0 °C(Predicted) |
Solubility | DMSO: soluble15mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | 9.59±0.10(Predicted) |
Storage Condition | 2-8°C |
In vitro study | Dimethylenastron is a potent Eg5 inhibitor, with an IC 50 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. |
In vivo study | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.491 ml | 17.455 ml | 34.91 ml |
5 mM | 0.698 ml | 3.491 ml | 6.982 ml |
10 mM | 0.349 ml | 1.745 ml | 3.491 ml |
5 mM | 0.07 ml | 0.349 ml | 0.698 ml |
biological activity | Dimethylenastron is an effective, specific and reversible kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) inhibitor with an IC50 value of 200 nM. Dimethylenastron can induce mitotic arrest and apoptosis of human multiple myeloma cells and up-regulate Hsp70 expression. |
target | TargetValue KSP (Cell-free say) 200 nM |
Target | Value |
KSP (Cell-free assay) | 200 nM |
in vitro study | Dimethylenastron is a potent Eg5 inhibitor, with an IC 50 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 μ m) uses accumulation of cells in G2/m in HeLa cells. Dimethylenastron (3 and 10 μ m) 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. |
in vivo study | 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. |