ML141

Catalog No.S7686 Synonyms: CID-2950007

ML141 Chemical Structure

Molecular Weight(MW): 407.49

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).

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3 Customer Reviews

  • (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.

    J Virol, 2016, doi: 10.1128/JVI.01916-16. . ML141 purchased from Selleck.

    Western blot analysis of expressions of E-cadherin and vimentin in HCT116 cells treated with ML141 compared with DMSO-treated cells

    J Proteome Res, 2018, 17(1):265-275. ML141 purchased from Selleck.

    Compared with the DMSO group, there were low levels of (D) MMP-9 and (E) MMP-2 expression in the ML141-treated group. There were no statistically significant differences in MMP-9 and MMP-2 expression between ML14-treated and ML141+TAOCSB-treated groups. *P<0.05 or **P<0.01 vs. DMSO group. TAOCSB, total alkaloids of Corydalis saxicola bunting; MMP, matrix metalloproteinase; Cdc42, cell division cycle 42; DMSO, dimethylsulfoxide.

    ONCOLOGY LETTERS, 2018, 15: 475-482. ML141 purchased from Selleck.

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Biological Activity

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).
Targets
cdc42 [1]
200 nM
In vitro

ML141 enhances the ability of TMX to suppress BLBC cell growth through both induction of cell death and suppression of cell division. [2] ML141 also significantly protects neuroblastoma cells from metformin-induced apoptosis. [3] Moreover, ML141 diminishes K. pneumoniae invasion in a dose-dependent manner. [4]

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. [2] In addition, ML141 (10 mg/kg i.p.) enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization in mice. [5]

Protocol

Kinase Assay:

[1]

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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 Research:

[2]

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  • Cell lines: Basal-B (MDA-MB 231 and HCC38) and Basal-A with HER2 amplification (HCC1954) cells
  • Concentrations: ~20 μM
  • Incubation Time: 48 hours
  • Method:

    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)
Animal Research:

[2]

+ Expand
  • Animal Models: NOD/SCID mice bearing MDA-MB 231 derived tumors
  • Formulation: Corn oil
  • Dosages: 1 mg/day
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL warmed (198.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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.

Chemical Information

Molecular Weight 407.49
Formula

C22H21N3O3S

CAS No. 71203-35-5
Storage powder
Synonyms CID-2950007

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID