Hepln-13

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Chemical Structure| 64369-13-7 同义名 : -
CAS号 : 64369-13-7
货号 : A1497219
分子式 : C17H13BrN2
纯度 : 99%+
分子量 : 325.2
MDL号 : MFCD01038678
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(184.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Hepsin is a membrane serine protease expressed in several human tissues including the liver, kidney, prostate, and thyroid. In vitro studies have shown that hepsin activates blood clotting factors VII, XII, and IX, pro-urokinase (pro-uPA), and pro-hepatocyte growth factor (pro-HGF)[1]. Hepsin expression was upregulated in prostate cancer tissue samples and cell lines. Inhibition of hepsin attenuated EMT and cell invasion and downregulated the expression of miR-222. Decreased miR-222 expression enhanced the level of PPP2R2A, which in turn attenuated the AKT signaling. Activation of miR-222 or AKT could block the inhibitory effects on EMT and cell invasion induced by hepsin deficiency[2]. Hepsin-induced depletion of cellular HAI-1 led to a sharp increase in pericellular serine protease activity. The derepressed hepsin proteolytically activated downstream serine proteases, augmented HGF/MET signalling and caused deterioration of desmosomes and hemidesmosomes; structures important for cell cohesion and cell-basement membrane interaction[3]. Hepsin expression was found to be significantly higher in endometrial cancer compared to normal endometrium and endometrial hyperplasia. High levels of hepsin expression were associated with advanced stage (p<0.001), high grade (p=0.002), depth of myometrial invasion (p<0.001), cervical involvement (p=0.007), lymph node metastasis (p=0.001), lymph vascular space (LVS) involvement (p=0.006), ovarian metastasis (p=0.002), and peritoneal cytology (p=0.03) of endometrial cancer[4]. Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer. Hepln-13 (10 µM; 2 hours; 293 cells) inhibits cleavage. HepIn-13 displays dose dependent inhibition of Hepsin overexpression-relevant prostate cancer phenotypes and blocks prostate cancer metastasis[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.38mL

3.08mL

1.54mL

30.75mL

6.15mL

3.08mL
参考文献

[1] Qingyu Wu, Gordon Parry. Hepsin and prostate cancer. Front Biosci. 2007 Sep 1;12:5052-9.

[2]Ruiqian Li,et al. Hepsin Promotes Epithelial-Mesenchymal Transition and Cell Invasion Through the miR-222/PPP2R2A/AKT Axis in Prostate Cancer. Onco Targets Ther. 2020 Nov 24;13:12141-12149.

[3]T A Tervonen,et al. Deregulated hepsin protease activity confers oncogenicity by concomitantly augmenting HGF/MET signalling and disrupting epithelial cohesion. Oncogene. 2016 Apr 7;35(14):1832-46.

[4]Tamaki Matsuo,et al. Expression of the serine protease hepsin and clinical outcome of human endometrial cancer. Anticancer Res. Jan-Feb 2008;28(1A):159-64.

[5]Tang X, et al. Targeted inhibition of cell-surface serine protease Hepsin blocks prostate cancer bone metastasis. Oncotarget. 2014;5(5):1352-1362.