| Name | BMS-3 |
| Description | BMS-3 is a potent LIMK inhibitor with IC50 values of 5 nM and 6 nM for LIMK1 and LIMK2, respectively. |
| 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] |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.66 mM), Sonication is recommended.
DMSO : 27.5 mg/mL (64.06 mM), Sonication is recommended.
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| Keywords | LIMKs | LIMKinase | LIMK2 | LIMK1 | LIM Kinase (LIMK) | LIM Kinase | Inhibitor | inhibit | BMS-3 | BMS3 | BMS 3 |
| Inhibitors Related | BMS-5 | CRT-0105950 | LX7101 | TH-257 | SM1-71 | TH-263 | LIMK1 inhibitor 2 | T56-LIMKi | GLPG3312 | R-10015 | LIMK-IN-22j | LX-7101 hydrochloride |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Fluorochemical Library | Anti-Cancer Compound Library |
United States
