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 (warmed with 50ºC water bath) 81 mg/mL (198.77 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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.

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] This compound also significantly protects neuroblastoma cells from metformin-induced apoptosis. [3] Moreover, it 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, this compound (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 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.
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/21433396/
  • https://pubmed.ncbi.nlm.nih.gov/23606532/
  • https://pubmed.ncbi.nlm.nih.gov/25365944/
  • https://pubmed.ncbi.nlm.nih.gov/25452552/
  • https://pubmed.ncbi.nlm.nih.gov/25315193/

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：

IGSF10 is a RET antagonist regulating Ewing sarcoma growth and GnRH neuron migration [ Cell Rep, 2025, 44(8):116025] PubMed: 40700020
PI(3,4,5)P3-mediated Cdc42 activation regulates macrophage podosome assembly [ Cell Mol Life Sci, 2025, 82(1):127] PubMed: 40126693
CDC42 supports HBV entry by NTCP translocation to the plasma membrane and macropinocytosis [ EMBO Rep, 2025, 26(21):5239-5269] PubMed: 40954218
Cdc42 is crucial for the early regulation of hepatic stellate cell activation [ Am J Physiol Cell Physiol, 2025, 10.1152/ajpcell.00987.2024] PubMed: 39871537
Role of membrane proximal actin regulators in SARS-CoV-2 spike-induced cell-cell fusion [ Biochem Biophys Res Commun, 2025, 766:151846] PubMed: 40300332
Vav2 is a master regulator of repair against bacterial pore-forming toxins [ bioRxiv, 2025, 2025.07.31.668026] PubMed: 40766405
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

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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