• 产品描述： MZ-1 是一种 bromodomain-containing protein 4 (BRD4) 的PROTAC降解剂。MZ-1 可结合到Brd结构域Brd2BD1、Brd2BD2、Brd3BD1、Brd3BD2、Brd4BD1和Brd4BD2，对应的Kd值分别为62 nM、60 nM、21 nM、13 nM、39 nM和15 nM

• 靶点： Brd3(BD2)(Cell-free assay):13 nM(Kd); Brd4(BD2)(Cell-free assay):15 nM(Kd); Brd3(BD1)(Cell-free assay):21 nM(Kd); Brd4(BD1)(Cell-free assay):39 nM(Kd); Brd2(BD2)(Cell-free assay):60 nM(Kd);Brd2(BD1):62 nM(Kd);EpigeneticReaderDomain

• 体外研究：
  MZ-1 induces apoptosis of ovarian cancer cells and inhibits periostin-mediated ovarian cancer cell migration and invasion in vitro. MZ-1 specifically and efficiently inhibits the colony formation of periostin cells in soft agar, which clearly indicates a proproliferation role of periostin

• 体内研究：
  Our in vivo studies shows significant growth inhibition by MZ-1 on both subcutaneous and intraperitoneal (i.p.) tumors derived from the periostin-expressing ovarian cancer cell line A2780. In addition, MZ-1 treatment leads to a reduction of the metastatic potential of these A2780 i.p. tumors. The in vivo antitumor effects of MZ-1 are linked to its specific inhibition of anchorage-independent growth and survival of periostin-expressing cells, as well as its neutralizing effects on periostin-induced cancer cell migration and invasion

• 细胞实验： Cell lines: A2780, OAW-42, SKOV-3, TOV-112D, ES2, SP2/0 cell line Concentrations: 20 μM Incubation Time: 2 and 4 days Method: In vitro apoptosis assay: Cells are grown in 24-well plates in serum-free medium (SFM) plus 1% BSA overnight to reach 50% to 60% confluency. A portion of 20 mg/mL of MZ-1 or control antibody is added into the wells. Cell apoptosis is analyzed 2 and 4 days later by using Annexin V-FITC Apoptosis Detection Kit. The cell flow cytometry is carried on Cell LabQuanta SC.

• 动物实验： Animal Models: Female SCID beige mice (6-8 weeks old) with A2780/TOV-112D xenografts Dosages: 20 mg/kg Administration: IH/SC, IP

• 参考文献：
  1. Morgan S Gadd, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521. 2. Min Zhu, et al. Neutralizing monoclonal antibody to periostin inhibits ovarian tumor growth and metastasis. Mol Cancer Ther. 2011 Aug;10(8):1500-8.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0.997 ml	4.987 ml	9.974 ml
  5 mM	0.199 ml	0.997 ml	1.995 ml
  10 mM	0.1 ml	0.499 ml	0.997 ml
  50 mM	0.02 ml	0.1 ml	0.199 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *