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BMS-3 is a potent LIMK inhibitor with IC50 values of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $45 | In Stock | |
10 mg | $71 | In Stock | |
25 mg | $146 | In Stock | |
50 mg | $243 | In Stock | |
100 mg | $353 | In Stock | |
1 mL x 10 mM (in DMSO) | $45 | In Stock |
Description | BMS-3 is a potent LIMK inhibitor with IC50 values of 5 nM and 6 nM for LIMK1 and LIMK2, respectively. |
Targets&IC50 | LIMK2:6 nM, LIMK1:5 nM |
In vitro | BMS-3 (Compound 2) exhibits a dose-dependent decrease in A549 human lung cancer cell viability by inducing mitotic arrest, characterized by enhanced total nuclear DNA intensity and histone H3 phosphorylation following a 24-hour exposure. It effectively inhibits these cells with an EC50 value of 154 nM[1]. Additionally, BMS-3 elucidates the role of LIMK1 in Cofilin phosphorylation; inhibition of p-LIMK by BMS-3 (1-50 μM) leads to a notable reduction in p-Cofilin levels after a 10-minute incubation under capacitating conditions, with a marked decrease in actin polymerization levels compared to the DMSO controls. Furthermore, under capacitating conditions, mouse sperm exposure to escalating concentrations of BMS-3 (0, 1, 10, and 50 μM) for 90 minutes significantly diminishes the percentage of sperm undergoing acrosomal exocytosis upon Progesterone stimulation[2], highlighting BMS-3's potential in affecting sperm functionality. |
Kinase Assay | The protein kinase domains of human LIMK1 and LIMK2 are expressed as glutathione S-transferase fusion proteins using the Bac-to-Bac system in Sf9 cells. Compounds 1 to 6 (e.g., BMS-3) are assayed for inhibition of LIMK1 and LIMK2 protein kinase activity by radioactive phosphate incorporation into biotinylated full-length human destrin. Reactions are done with a concentration series of compound in 25 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 5 mM MnCl2, 1 μM total ATP, 83 μg/mL biotinylated destrin, 167 ng/mL glutathione S-transferase-LIMK1, or 835 ng/mL glutathione S-transferase-LIMK2 in a total volume of 60 μL at room temperature for 30 min (LIMK1) or 60 min (LIMK2). Reactions are terminated by addition of 140 μL of 20% TCA/100 mM sodium pyrophosphate, and the precipitates are harvested onto GF/C unifilter plates. The radioactivity incorporated is determined using a TopCount after addition of 35 μL Microscint scintillation fluid[1] |
Molecular Weight | 429.27 |
Formula | C17H12Cl2F2N4OS |
Cas No. | 1338247-30-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 27.5 mg/mL (64.06 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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