ML 141

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ML 141

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	71203-35-5
包装:	10mg
市场价:	1080元

产品介绍

ML 141 (CID-2950007) 是一种有效的、变构的、选择性的和可逆的 Cdc42 GTPase 非竞争性抑制剂。 ML 141 抑制 Cdc42 野生型和 Cdc42 Q61L 突变体，EC50 分别为 2.1 和 2.6 μM。 ML 141 对 GTP 酶 Rho 家族的其他成员（Rac1、Rab2、Rab7）显示出低微摩尔效力和选择性。 ML 141 在多个细胞系中不显示细胞毒性。

Cas No.	71203-35-5
别名	CID-2950007
化学名	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
分子式	C₂₂H₂₁N₃O₃S
分子量	407.49
溶解度	DMF: 30 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL,DMSO: 20 mg/mL
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.