Dimethylenastron
Dimethylenastron
CAS: 863774-58-7
Molecular Formula: C16H18N2O2S
Dimethylenastron - Names and Identifiers
Dimethylenastron - Physico-chemical Properties
| 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. |
Dimethylenastron - Risk and Safety
| WGK Germany | 3 |
Dimethylenastron - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
Dimethylenastron - Reference Information
| 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. |
Last Update：2024-04-10 22:29:15
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