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PTP1B Inhibitor (CAS 765317-72-4) - chemical structure image
PTP1B Inhibitor 的分子结构, CAS编号: 765317-72-4
PTP1B Inhibitor (CAS 765317-72-4) - chemical structure image
PTP1B Inhibitor 的分子结构, CAS编号: 765317-72-4
PTP1B Inhibitor 的分子结构, CAS编号: 765317-72-4

PTP1B Inhibitor 抑制剂 (CAS 765317-72-4)

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查看产品引用文献(13)

备用名:
PTP1B Inhibitor is also known as Protein Tyrosine Phosphatase 1B Inhibitor.
应用:
PTP1B Inhibitor 是一种具有细胞渗透性的 PTP1B（蛋白酪氨酸磷酸酶 1B）异位抑制剂。
CAS号码:
765317-72-4
纯度:
≥95%
分子量:
741.5
分子式:
C26H19Br2N3O7S3
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

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PTP1B抑制剂可抑制蛋白酪氨酸磷酸酶1B的活性，而蛋白酪氨酸磷酸酶1B是胰岛素和瘦素信号通路负调控的关键因素。分子动力学研究表明，由于在活性位点周围形成了氢键网络，PTP1B抑制剂具有强结合和高选择性。如果PTP1B在CHO和HEK293稳定细胞克隆中过表达，则在整个克隆生成和维持过程中会导致细胞毒性低和复苏率低。研究表明，PTP1B抑制剂可以显著放大PTP1B过表达的CHO细胞中关键葡萄糖转运蛋白Glut4的膜转位。PTP1B抑制剂选择性增加胰岛素受体、胰岛素受体底物1和Akt的磷酸化，模拟胰岛素的作用。PTP1B抑制剂也称为蛋白酪氨酸磷酸酶1B抑制剂，化学名称为3-(3,5-二溴-4-羟基苯甲酰)-2-乙基-N-[4-[(2-噻唑基氨基)磺酰基]苯基]-6-苯并呋喃磺酰胺。


PTP1B Inhibitor 抑制剂 (CAS 765317-72-4) 参考文献

  1. 从新型组合库和筛选程序中获得特异性强效 PTP1B 抑制剂。  |  Shen, K., et al. 2001. J Biol Chem. 276: 47311-9. PMID: 11584002
  2. Hyrtiosal是一种来自海洋海绵Hyrtios erectus的PTP1B抑制剂，对PI3K/AKT活化, 葡萄糖转运和TGFbeta/Smad2信号转导具有广泛的细胞效应。  |  Sun, T., et al. 2007. Chembiochem. 8: 187-93. PMID: 17183521
  3. 作为药物靶点的 PTP1B：PTP1B 抑制剂发现的最新进展。  |  Zhang, S. and Zhang, ZY. 2007. Drug Discov Today. 12: 373-81. PMID: 17467573
  4. 通过高通量筛选发现新型 PTP1B 竞争性抑制剂。  |  Shi, L., et al. 2008. Acta Pharmacol Sin. 29: 278-84. PMID: 18215359
  5. PTP1B 与阻抑剂相互作用的分子动力学研究：从第一个磷酸盐结合位点到第二个位点。  |  Wang, JF., et al. 2009. Protein Eng Des Sel. 22: 349-55. PMID: 19380334
  6. 绞股蓝中的达玛烷及其衍生物作为蛋白酪氨酸磷酸酶 1B 抑制剂的合成。  |  Xu, JQ., et al. 2010. Bioorg Med Chem. 18: 3934-9. PMID: 20472439
  7. 杆状病毒表达系统：生产具有催化活性的人类 PTP-1B 的替代方法。  |  Sundaram, S., et al. 2010. Mol Biol (Mosk). 44: 535-40. PMID: 20608179
  8. 从濒危植物杜鹃花（Rhododendron brachycarpum G. Don.  |  Choi, YH., et al. 2012. Bioorg Med Chem Lett. 22: 6116-9. PMID: 22940448
  9. 海南软珊瑚 Sarcophyton trocheliophorum Marenzeller 中作为 PTP1B 抑制剂的前所未有的二萜类化合物。  |  Liang, LF., et al. 2013. Org Lett. 15: 274-7. PMID: 23273218
  10. 肌动蛋白结合蛋白 Mena 对受体酪氨酸激酶信号传导的 PTP1B 依赖性调控。  |  Hughes, SK., et al. 2015. Mol Biol Cell. 26: 3867-78. PMID: 26337385
  11. PTP1B 抑制剂通过激活 DOCK180/Rac1 通路促进内皮细胞的运动。  |  Wang, Y., et al. 2016. Sci Rep. 6: 24111. PMID: 27052191
  12. 一种从灵芝中提取的新型 PTP1B 抑制剂可通过调节胰岛素信号通路中的 IRS1-GLUT4 级联来改善胰岛素抵抗。  |  Yang, Z., et al. 2018. Food Funct. 9: 397-406. PMID: 29215104
  13. PTP1B 抑制剂 Claramine 可修复糖尿病诱导的小鼠空间学习和记忆损伤。  |  Wu, M., et al. 2023. Mol Neurobiol. 60: 524-544. PMID: 36319905

订购信息

产品名称产品编号规格价格数量收藏夹

PTP1B Inhibitor, 5 mg

sc-222227
5 mg
RMB2550.00

PTP1B Inhibitor, 25 mg

sc-222227A
25 mg
RMB10357.00

What is the IC50 of this product? The website has two different numbers and I am not sure what they designate.

Asked by: SCchem16
Thank you for your question. This chemical, PTP1B Inhibitor: sc-222227, is a non-competitive allosteric inhibitor of PTP1B (IC50 = 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively). There are two IC50 values because the inhibitory concentration was measured at two different (assumed) amino acids.
Answered by: Chemical Support 2
Date published: 2017-03-10

What is the half-life period of sc-222227?

Asked by: SCchem16
Thank you for your question. This chemical, PTP1B Inhibitor (CAS 765317-72-4), has a half-life of > 3 years if storage conditions are kept.
Answered by: Chemical Support 2
Date published: 2017-03-10
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Rated 5 out of 5 by from Inibitore allosterico della PTP1BIl prodotto è stato consegnato rapidamente; la confezione era integra e il prodotto ben conservato. In fase di prove sperimentali, il prodotto è risultato attivo e conforme alle aspettative.
Date published: 2023-02-06
Rated 5 out of 5 by from HughesHughes, SK. et al. (PubMed 26337385) report that Mena associates constitutively with the tyrosine phosphatase PTP1B and mediates a novel negative feedback mechanism that attenuates receptor tyrosine kinase signaling. They also found that disruption of this attenuation by MenaINV sensitizes tumor cells to low growth factor concentrations, thereby increasing the migration and invasion responses that contribute to aggressive, malignant cell phenotypes. -SCBT Publication Review
Date published: 2015-05-26
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PTP1B Inhibitor 抑制剂 is rated 5.0 out of 5 by 2.
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