|-- -- --|
|Solubility (25°C) *||In vitro||DMSO||81 mg/mL warmed (198.77 mM)|
|In vivo||2% DMSO+30% PEG 300+5% Tween 80+ddH2O||10mg/mL|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).|
|In vitro||ML141 enhances the ability of TMX to suppress BLBC cell growth through both induction of cell death and suppression of cell division.  ML141 also significantly protects neuroblastoma cells from metformin-induced apoptosis.  Moreover, ML141 diminishes K. pneumoniae invasion in a dose-dependent manner. |
|In vivo||In NOD/SCID mice bearing MDA-MB 231 derived tumors, ML141 (1 mg/day i.p.), via inhibition of Cdc42, enables TMX to suppress growth of MDA-MB 231 derived tumors.  In addition, ML141 (10 mg/kg i.p.) enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization in mice. |
|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.|
|Cell lines||Basal-B (MDA-MB 231 and HCC38) and Basal-A with HER2 amplification (HCC1954) cells|
|Incubation Time||48 hours|
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.
|Animal Models||NOD/SCID mice bearing MDA-MB 231 derived tumors|
Data from [Data independently produced by , , J Virol, 2016, doi: 10.1128/JVI.01916-16. ]
(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
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