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NSC 405020

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Chemical Structure| 7497-07-6 同义名 : -
CAS号 : 7497-07-6
货号 : A160858
分子式 : C12H15Cl2NO
纯度 : 98%
分子量 : 260.16
MDL号 : MFCD02006898
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: 250 mg/mL(960.95 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：

1% DMSO+30% polyethylene glycol+1% Tween 80+water 5 mg/mL

生物活性
靶点

  • MMP
描述 NSC405020 is a PEX inhibitor. NSC405020 repressed migration of 184B5-MT cells on COL-I in a dose-dependent manner at concentration ranging in 25-100μM. It directly interacted with PEX in the full-length MT1-MMP structure and that these interactions affected PEX homodimerization. NSC405020 did not inhibit the catalytic function of cellular MT1-MMP or the catalytic activity of MMP-2. NSC 405020 at concentration of 400μM did not show any cytotoxicity in MCF7-β3/MT cells in vitro. However, injection with NSC405020 at 0.5mg/kg 3 times per week for 7 injections inhibited MCF7-β3/MT tumor growth in vivo, and repressed the collagenolytic function of PEX[2].
作用机制 Binding of NSC405020 affected the conformation and flexibility of blades I to IV of the β-propeller and, as a result, decreased the PEX-dependent homodimerization of cellular MT1-MMP.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.84mL

0.77mL

0.38mL

19.22mL

3.84mL

1.92mL

38.44mL

7.69mL

3.84mL
参考文献

[1]Remacle AG, Golubkov VS, et al. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49.

[2]Remacle AG, Golubkov VS, Shiryaev SA, Dahl R, Stebbins JL, Chernov AV, Cheltsov AV, Pellecchia M, Strongin AY. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49. doi: 10.1158/0008-5472.CAN-11-4149. Epub 2012 Mar 9. PMID: 22406620; PMCID: PMC3342448.