产品说明书

ML141

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Chemical Structure| 71203-35-5 同义名 : CID-2950007
CAS号 : 71203-35-5
货号 : A201975
分子式 : C22H21N3O3S
纯度 : 99%+
分子量 : 407.485
MDL号 : MFCD05987165
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 55 mg/mL(134.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

生物活性
靶点

  • Cdc42-subclass

    cdc42, IC50:200 nM
描述 Cdc42, a member of the Rho family of GTPases, has been shown to play a role in cell adhesion, cytoskeletal arrangement, phagocytosis and cell motility and migration. ML141 is a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase with low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7)[3]. Pharmacological inhibition of Cdc42 with ML141 was similarly effective as genetic knockdown at enabling TMX-induced reductions in levels of EGFR (epidermal growth factor receptor). Co-exposure to 20 µM ML141 (a concentration that selectively inhibits Cdc42 function in BLBC cells) enabled TMX (tamoxifen) to cause a ∼45% reduction in EGFR levels. ML141 exposure also enhanced the ability of TMX to suppress BLBC cell growth, through both induction of cell death and suppression of cell division. Tumour bearing animals were treated with 1 mg/day ML141 and 125 µg/day TMX. Pharmacological inhibition of Cdc42 with ML141 enabled TMX to suppress growth of MDA-MB 231 derived tumours. Moreover, the tumour sizes resulting from ML141 pre-treated cells were markedly smaller than those of the control group[4]. Moreover, both the absolute numbers of KL (Lin− c-Kit+ sca-1−) and KSL (Lin− c-Kit+ sca-1+) population in ML141 treated mice were increased as compared to these in DMSO vehicle control mice. Mice treated with 10 μg ML141 presented higher KL and KSL counts than those in mice with 5 μg ML141[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.54mL

4.91mL

2.45mL
参考文献

[1]Chen C, Song X, et al. Cdc42 inhibitor ML141 enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization. Int J Hematol. 2015 Jan;101(1):5-12.

[2]Kumar A, Al-Sammarraie N, et al. Metformin impairs Rho GTPase signaling to induce apoptosis in neuroblastoma cells and inhibits growth of tumors in the xenograft mouse model of neuroblastoma. Oncotarget. 2014 Nov 30;5(22):11709-22.

[3]Surviladze Z, Waller A, Strouse JJ, et al. A Potent and Selective Inhibitor of Cdc42 GTPase. In: Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010

[4]Chen HY, Yang YM, Stevens BM, Noble M. Inhibition of redox/Fyn/c-Cbl pathway function by Cdc42 controls tumour initiation capacity and tamoxifen sensitivity in basal-like breast cancer cells. EMBO Mol Med. 2013;5(5):723‐736

[5]Chen C, Song X, Ma S, et al. Cdc42 inhibitor ML141 enhances G-CSF-induced hematopoietic stem and progenitor cell mobilization. Int J Hematol. 2015;101(1):5‐12