ML141

製品コードS7686 バッチS768602

印刷

化学情報

Chemical Structure Synonyms CID-2950007 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H21N3O3S
分子量 407.49 CAS No. 71203-35-5
Solubility (25°C)* 体外 DMSO 81 mg/mL warmed with 50ºC water bath (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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Basal-B (MDA-MB 231 and HCC38) and Basal-A with HER2 amplification (HCC1954) cells
濃度 ~20 μM
反応時間 48 hours
実験の流れ

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.
動物実験 動物モデル NOD/SCID mice bearing MDA-MB 231 derived tumors
投薬量 1 mg/day
投与方法 i.p.

カスタマーフィードバック

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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
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
NELL2-cdc42 signaling regulates BAF complexes and Ewing sarcoma cell growth [ Cell Rep, 2021, 36(1):109254] PubMed: 34233189
TSH activates macrophage inflammation by G13 and G15-dependent pathways [ Endocrinology, 2021, bqab077] PubMed: 33851697
The fibrillin-1 RGD motif posttranscriptionally regulates ERK1/2 signaling and fibroblast proliferation via miR-1208 [ FASEB J, 2021, 35(5):e21598] PubMed: 33871068

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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