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• 产品描述： XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity

• 靶点： BMK1:80 nM (Kd);BRD4:190 nM (Kd);ERK; BMI-1; EpigeneticReaderDomain

• 体外研究：
  XMD8-92 (0-5 Μm; 48 hours) inhibits the proliferation of HMEC and cancer cells.
  XMD8-92 effectively inhibits BMK1 activation as well as induces PML’s (promyelocytic leukemia protein) downstream effector, p21. XMD8-92 significantly inhibits basic fibroblast growth factor (bFGF) induced angiogenesis in Matrigel plugs. XMD8-92 significantly induces p21 expression in HeLa and A549 cells. Cell Viability Assay Cell Line: HMEC, A549 and HeLa cells Concentration: 0.16, 0.32, 0.63, 1.25, 2.5 or 5 μM Incubation Time: 48 hours Result: Inhibited the proliferation of HMEC and cancer cells.

• 体内研究：
  XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors. Animal Model: HeLa Xenograft Model (6-week-old Nod/Scid mice)[1] Dosage: 50 mg/kg Administration: I.p.; twice a day for 28 days Result: Significantly inhibited the growth of the xenografted human tumors.

• 参考文献：
  1. Yang Q, et al. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.Cancer Cell. 2010 Sep 14;18(3):258-67. 2. Yang Q, et al. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011 Jun 1;17(11):3527-32. 3. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016;113(42):11865-11870. 4. Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7(349):ra102.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.107 ml	10.536 ml	21.072 ml
  5 mM	0.421 ml	2.107 ml	4.214 ml
  10 mM	0.211 ml	1.054 ml	2.107 ml
  50 mM	0.042 ml	0.211 ml	0.421 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 *