ML141

Catalog No.S7686 Batch:S768601

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Technical Data

Formula

C22H21N3O3S
Molecular Weight 407.49 CAS No. 71203-35-5
Solubility (25°C)* In vitro DMSO 81 mg/mL (198.77 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[2]
  • 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.
Animal Study:

[2]
  • Animal Models

    NOD/SCID mice bearing MDA-MB 231 derived tumors

  • Dosages

    1 mg/day

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , J Virol, 2016, doi: 10.1128/JVI.01916-16. ]

Data from [Data independently produced by , , J Proteome Res, 2018, 17(1):265-275]

Data from [Data independently produced by , , ONCOLOGY LETTERS, 2018, 15: 475-482]

Selleck's ML141 has been cited by 32 publications

Proangiogenic effect and underlying mechanism of holmium oxide nanoparticles: a new biomaterial for tissue engineering [ J Nanobiotechnology, 2024, 22(1):357] PubMed: 38902755
Dennd2c Negatively Controls Multinucleation and Differentiation in Osteoclasts by Regulating Actin Polymerization and Protrusion Formation [ Int J Mol Sci, 2024, 25(21)11479] PubMed: 39519032
Roles of USP1 in Ewing sarcoma [ Genes Cancer, 2024, 15:15-27] PubMed: 38323120
SAMHD1-induced endosomal FAK signaling promotes human renal clear cell carcinoma metastasis by activating Rac1-mediated lamellipodia protrusion [ Exp Mol Med, 2023, 55(4):779-793] PubMed: 37009792
Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749] PubMed: 37100284
Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749] PubMed: 37100284
CIP4 targeted to recruit GTP-Cdc42 involving in invadopodia formation via NF-κB signaling pathway promotes invasion and metastasis of CRC [ Mol Ther Oncolytics, 2022, 24:873-886] PubMed: 35317515
Lovastatin Inhibits RhoA to Suppress Canonical Wnt/β-Catenin Signaling and Alternative Wnt-YAP/TAZ Signaling in Colon Cancer [ Cell Transplant, 2022, 31:9636897221075749] PubMed: 35168393
Pressure and stiffness sensing together regulate vascular smooth muscle cell phenotype switching [ Sci Adv, 2022, 8(15):eabm3471] PubMed: 35427166
Slit2 signaling stimulates Ewing sarcoma growth [ Genes Cancer, 2022, 13:88-99] PubMed: 36533189

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.