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BMS-5 (LIMKi 3) is a potent LIM kinase inhibitor (IC50 values are 7 and 8 nM for LIMK1 and LIMK2 respectively). BMS-5 inhibits cofilin phosphorylation in MDA-MB-231 breast cancer cells. BMS-5 reduces MDA-MB-231 tumor cell invasion in a 3D matrigel invasion assay. COCs exhibited different diffusion situation between control and treatment group: the diffusion of 200 µM BMS-5 (LIMKi 3) treated-COCs was significantly weaker than the control group. In the standard of COCs surrounded by the cumulus cell layers, we counted the proportion of diffusion and found that the rate of good diffusion was decreased significantly (40.05 ± 3.03% vs. 20.50 ± 4.05%; p < 0.05). Oocytes were then obtained from COCs after hyaluronidase treatment, we found that few oocytes extruded the polar body after 200 µM BMS-5 (LIMKi 3) treatment.
| Cell Experiment | |
|---|---|
| Cell lines | COCs |
| Preparation method | For LIMK1/2 inhibitor treatment, stock LIMKi 3 (50 mM in dimethylsulfoxide (DMSO)) was diluted in M199 to final concentrations of 50, 100, 150 and 200 µM. A control group was cultured in DMSO at the same relative concentration of solvent. COCs were cultured with LIMKi 3 to evaluate its effects on oocyte maturation. COCs were denuded of their cumulus cells by gentle pipetting with 0.1% (w/v) hyaluronidase. |
| Concentrations | 200 µM |
| Incubation time | 44 h |
| Animal Experiment | |
|---|---|
| Animal models | NF1+/− mice |
| Formulation | DMEM × 1 containing 5% FCS |
| Dosages | 0, 25 or 50 μM |
| Administration | i.v. |
| Molecular Weight | 431.29 |
| Formula | C17H14Cl2F2N4OS |
| CAS Number | 1338247-35-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Jia RX, et al. PeerJ. LIMK1/2 inhibitor LIMKi 3 suppresses porcine oocyte maturation.
| Related LIM Kinase Products |
|---|
| 8beta,9alpha-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility. |
| LIMK-IN-1
LIMK-IN-1 is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. |
| Curcolonol
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer. |
| CRT 0105446
CRT 0105446 (compound 22d) is a LIMK1 inhibitor, with an IC50 of 8 nM. |
| CRT0105950
CRT0105950 is a potent LIMK inhibitor, with IC50s of 0.3 nM and 1 nM for LIMK1 and LIMK2 respectively. CRT0105950 can be used for the research of cancer. |
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