Molecular Formula | C17H12Cl2F2N4OS |
Molar Mass | 429.27 |
Density | 1.69±0.1 g/cm3(Predicted) |
pKa | 8.28±0.70(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
In vitro study | BMS-3 (Compound 2) causes a dose-dependent reduction in cell count and induces mitotic arrest by increases in total nuclear DNA intensity and histone H3 phosphorylation after 24 h treatment in A549 human lung cancer cells. BMS-3 inhibits A549 human lung cancer cells with EC 50 value of 154 nM. BMS-3 is used to demonstrate the direct participation of LIMK1 in the phosphorylation of Cofilin. Inhibition of p-LIMK with 1-50 μM of BMS-3 results in a dose-dependent decrease of p-Cofilin after 10 min incubation in capacitating conditions. As a control, sperm are also incubated for 10 min under non-capacitating conditions which result in low levels of p-Cofilin. In the presence of 1 or 50 μM of BMS-3, actin polymerization levels are significantly lower compared to controls (DMSO). Mouse sperm are incubated under capacitating conditions for 90 min in the presence or absence of increasing concentrations of p-LIMK inhibitor BMS-3 (0, 1, 10 and 50 μM). The increasing concentrations of BMS-3 result in a strong decrease on the percentage of sperm that undergoes acrosomal exocytosis after stimulation with 20 μM of Progesterone. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.33 ml | 11.648 ml | 23.295 ml |
5 mM | 0.466 ml | 2.33 ml | 4.659 ml |
10 mM | 0.233 ml | 1.165 ml | 2.33 ml |
5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
biological activity | BMS-3 is a highly effective LIMK inhibitor, inhibiting LIMK1 and LIMK2,IC50 is 5 nM and 6 nM respectively. |
target | LIMK1 5 nM (IC 50 ) LIMK2 6 nM (IC 50 ) |
in vitro study | BMS-3 (Compound 2) cause a dose-dependent reduction in cell count and induces mitotic arrest by increases in total nuclear DNA intensity and histone H3 phosphorylation after 24 h treatment in A549 human lung cancer cells. BMS-3 inhibits A549 human lung cancer cells with EC 50 value of 154 nM. BMS-3 is used to demonstrate the direct participation of LIMK1 in the phosphorylation of Cofilin. Inhibition of p-LIMK with 1-50μM of BMS-3 results in a dose-dependent decrease of p-Cofilin after 10 min incubation in capacitating conditions. As a control, sperm are also incubated for 10 min under non-capacitating conditions which result in low levels of p-Cofilin. In the presence of 1 or 50 μ m of BMS-3, actin polymerization levels are significantly lower compared to controls (DMSO). Mouse sperm are incubated under capacitating conditions for 90 min in the presence or absence of increasing concentrations of p-LIMK inhibitor BMS-3 (0,1, 10 and 50 μM). The increasing concentrations of BMS-3 result in a strong decrease on the percentage of sperm that undergoes acrosomal exocytosis after stimulation with 20 μM of Progesterone. |