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• 产品描述： K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer

• 靶点： Proteasome;Apoptosis;mTOR

• 体外研究：
  K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand[1].K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM. K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM. K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells. K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA. K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis. Cell Viability Assay Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 0-25 μM Incubation Time: 72 h Result: Inhibited MM cells growth. Apoptosis Analysis Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 10 μM Incubation Time: 48 h Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.

• 体内研究：
  K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo. K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection. Animal Model: ICR mice with IL-β or TNF-α injection Dosage: 30 mg/kg Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations. Animal Model: NOD/SCID mice with murine xenograft Dosage: 75 mg/kg Administration: Intraperitoneal injection; once daily for 14 days Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days. Animal Model: NOD/SCID mice with murine xenograft Dosage: 50 mg/kg Administration: Oral gavage; once daily for 14 days Result: Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.

• 参考文献：
  1. Umetani M, et al. A novel cell adhesion inhibitor, K-7174, reduces the endothelial VCAM-1 induction by inflammatory cytokines, acting through the regulation of GATA. Biochem Biophys Res Commun. 2000 Jun 7;272(2):370-4. 2. Imagawa S, et al. A GATA-specific inhibitor (K-7174) rescues anemia induced by IL-1beta, TNF-alpha, or L-NMMA. FASEB J. 2003 Sep;17(12):1742-4. 3. Kikuchi J, et al. The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602.

• 溶解性： Soluble  in  H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.558 ml	7.792 ml	15.584 ml
  5 mM	0.312 ml	1.558 ml	3.117 ml
  10 mM	0.156 ml	0.779 ml	1.558 ml
  50 mM	0.031 ml	0.156 ml	0.312 ml

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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 *