| Name | ML141 |
| Description | ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM). |
| Cell Research | Cells are incubated with 500 nM Calcein-AM and 1 µM PI for 15 min, after which live cells and dead cells (represented by positivity of Calcein-AM and PI staining, respectively) are counted utilizing the adherent cell Celigo™ cytometer. (Only for Reference) |
| Kinase Assay | Equilibrium binding assay : Wild-type GST-Cdc42 (4 μM) is bound to GSH-beads overnight at 4°C. Cdc42 on GSH-beads is depleted of nucleotide by incubating with 10 mM EDTA containing buffer for 20 min at 30°C, washing twice with NP- HPS buffer, then re-suspended in the same buffer containing 1 mM EDTA/or 1 mM MgCl2, 1 mM DTT and 0.1% BSA. Cdc42 unbound sites are blocked by incubation of protein–bead complex for 15 min at RT. Thirty μL of this suspension is incubated with 20 mM inhibitor for 3 min at RT and added 30 μL of various concentrations of ice cold BODIPY-FL-GTP. Samples incubated at 4° C for 45 min and binding of fluorescent nucleotide to enzyme is measured using an Accuri flow cytometer. Raw data are exported and plotted using GraphPad Prism software. |
| In vitro | In NOD/SCID mice carrying MDA-MB 231-derived tumors, ML141 (1 mg/day, intraperitoneally) inhibits the growth of these tumors by suppressing Cdc42, thereby enhancing the effectiveness of TMX. Additionally, ML141 (10 mg/kg, intraperitoneally) increases the mobilization of hematopoietic stem and progenitor cells induced by granulocyte colony-stimulating factors. |
| In vivo | ML141 significantly protects against apoptosis damage induced by metformin in neuroblastoma. It enhances the ability of caffeine to inhibit cell growth through the induction/suppression of cell death/division. Additionally, ML141 dose-dependently reduces the invasion of Klebsiella pneumoniae. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 125 mg/mL (306.76 mM), Sonication is recommended.
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| Keywords | toxicity | Ras | OVCA429 | ovarian | noncompetitive | ML-141 | ML141 | ML 141 | Inhibitor | inhibit | CID2950007 | CID 2950007 | cells | cdc42 | cancer | Apoptosis | anxiety | allosteric | acute |
| Inhibitors Related | Stavudine | Aceglutamide | Tamoxifen | Urea | Cysteamine hydrochloride | 2-Chloropyrazine | Gum arabic | Metronidazole | Citric Acid Triammonium | Dimethyl phthalate | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
