• 产品描述： Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors

• 体外研究： MDA-MB-468 细胞对 SuLfopin 表现出最显著的敏感性 (1、2.5 μM；4-8 天)。 SuLfopin (2 μM，HEK293 细胞；48 小时) 下调 Myc 转录。 SuLfopin (1、2.5 μM；PATU-8988T 细胞；4 天) 显示合成 (S) 期细胞数量小幅但显着减少，生长 1 (G1) 期细胞相应增加。 Cell Proliferation Assay Cell Line: Kuramochi, MDA-MB-468, NGP, NBL-S, MDA-MB-468 cells Concentration: 1, 2.5 μM Incubation Time: 4,6, 8 days Result: Showed variation in antiproliferative effects across cancer cell lines Kuramochi, MDA-MB-468, NGP and NBL-S, with the most pronounced sensitivity observed in MDA-MB-468 cells.

• 体内研究： SuLfopin (40 mg/kg; p.o.; QD/BID for 7 days) 使小鼠神经母细胞瘤消退。 SuLfopin (20-40 mg/kg; i.p.; daily for 27 days) 抑制小鼠胰腺癌的进展。 SuLfopin (25-100 μM) 可阻断斑马鱼的神经母细胞瘤。 Animal Model: Transgenic Th-MYCN mice Dosage: 40 mg/kg Administration: Once a day (QD) or twice a day (BID) for 7 days Result: Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.

• 参考文献：
  1. Dubiella C, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021;17(9):954-963.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0 ml	0 ml	0 ml
  5 mM	0 ml	0 ml	0 ml
  10 mM	0 ml	0 ml	0 ml
  50 mM	0 ml	0 ml	0 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 分子量 (g/mol)

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