Home Cell Cycle Rho inhibitor ML141 (CID-2950007)

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ML141 (CID-2950007) CDC42 Inhibitor

Cat.No.S7686

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.
ML141 (CID-2950007) Rho inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 407.49

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Quality Control

Batch: Purity: 99.77%
99.77

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
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Solubility

In vitro
Batch:

DMSO : 81 mg/mL (198.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 407.49 Formula

C22H21N3O3S

 Storage (From the date of receipt)
CAS No. 71203-35-5 Download SDF Storage of Stock Solutions

Synonyms CID-2950007 Smiles COC1=CC=C(C=C1)C2CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C4=CC=CC=C4

Mechanism of Action

Targets/IC50/Ki
cdc42
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. This compound also significantly protects neuroblastoma cells from metformin-induced apoptosis. Moreover, it diminishes K. pneumoniae invasion in a dose-dependent manner.
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 this compound 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 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, this compound (10 mg/kg i.p.) enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization in mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/25452552/
  • [5] https://pubmed.ncbi.nlm.nih.gov/25315193/

Applications

Methods Biomarkers Images PMID
Western blot E-cadherin / ROCK1 / ROCK2
S7686-WB1
30867745

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