Molecular Formula | C18H19NO3 |
Molar Mass | 297.35 |
Density | 1.11 |
Boling Point | 418.6±55.0 °C(Predicted) |
Solubility | DMSO: soluble5mg/mL (clear solution, warmed) |
Appearance | Yellow solid |
Color | white to beige |
Storage Condition | 2-8°C |
MDL | MFCD00534351 |
Use | Poloxin |
In vitro study | Poloxin (25 μM) induces defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC 50 of ∼4.8 μM. Poloxin exhibits a loose Plk1 PBD specificity with 4-10 times higher IC 50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains. |
In vivo study | Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231. |
Risk Codes | R43 - May cause sensitization by skin contact R50 - Very Toxic to aquatic organisms |
Safety Description | S36/37 - Wear suitable protective clothing and gloves. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.363 ml | 16.815 ml | 33.63 ml |
5 mM | 0.673 ml | 3.363 ml | 6.726 ml |
10 mM | 0.336 ml | 1.682 ml | 3.363 ml |
5 mM | 0.067 ml | 0.336 ml | 0.673 ml |
Biological activity | Poloxin is a non-competitive ATP inhibitor of Polo-like Kinase 1 (PLK1), which targets the polo-box domain, and the IC50 value is about 4.8 μM. |
target | PLK1 PBD 4.8 μM (IC 50 ) PLK2 PBD 18.7 μM (IC 50 ) PLK3 PBD 53.9 μM (IC 50 ) |
in vitro study | Poloxin (25 μM) induces defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC 50 of 4.8 μ m. Poloxin exhibits a loose plk1 PBD specificity with 4-10 times higher IC 50 values for plk2 and plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains. |
in vivo study | Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231. |