ML 141 (Synonyms: CID2950007) |
カタログ番号GC14800
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ML 141 (CID-2950007) は、Cdc42 GTPase の強力なアロステリックな選択的かつ可逆的な非競合的阻害剤です。 ML 141 は、Cdc42 野生型および Cdc42 Q61L 変異体をそれぞれ 2.1 および 2.6 μM の EC50 で阻害します。 ML 141 は、GTPase の Rho ファミリーの他のメンバー (Rac1、Rab2、Rab7) に対して低いマイクロモル効力と選択性を示します。 ML 141 は、複数の細胞株で細胞毒性を示しません。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 71203-35-5
Sample solution is provided at 25 µL, 10mM.
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ML141(CID-2950007) is a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase(IC50=200 nM) with low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). IC50 value: 200 nM [1]Target: Cdc42 inhibitorin vitro: In the primary HTS bead-based assay using 1 mM EDTA and 100 nM BODIPY-FL-GTP, potency for CID2950007 was IC50 = 2.6 and 5.4 μM for Cdc42 wild type and activated mutant, respectively [1]. ML141 exposure also enhanced the ability of TMX to suppress BLBC cell growth, through both induction of cell death and suppression of cell division [2]. in vivo: Treatment with ML141 + TMX caused a suppression of further tumour growth in vivo [2]. Parallel suppression of the conserved brain CDC42 activity by intracerebroventricular ML141 injection caused acute anxiety in mice [3]. using a pilocarpine-induced epileptic model, we found that pretreatment with ML141, a specific inhibitor of Cdc42, reduces seizure severity [4].
References:
[1]. Surviladze Z, et al. A Potent and Selective Inhibitor of Cdc42 GTPase. Probe Reports from the NIH Molecular Libraries Program
[2]. Chen HY, et al. 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 May;5(5):723-36.
[3]. Hanin G, et al. Competing targets of microRNA-608 affect anxiety and hypertension. Hum Mol Genet. 2014 Sep 1;23(17):4569-80.
[4]. Zhang Y, et al. Inhibition of the small GTPase Cdc42 in regulation of epileptic-seizure in rats. Neuroscience. 2015 Mar 19;289:381-91.
| Cas No. | 71203-35-5 | SDF | |
| 同義語 | CID2950007 | ||
| Chemical Name | 4-(5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide | ||
| Canonical SMILES | COC1=CC=C(C2CC(C3=CC=CC=C3)=NN2C4=CC=C(S(N)(=O)=O)C=C4)C=C1 | ||
| Formula | C22H21N3O3S | M.Wt | 407.49 |
| 溶解度 | DMF: 30 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL,DMSO: 20 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.454 mL | 12.2702 mL | 24.5405 mL |
| 5 mM | 490.8 μL | 2.454 mL | 4.9081 mL |
| 10 mM | 245.4 μL | 1.227 mL | 2.454 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)