Recombinant Active Human Hepsin His-tag Protein, CF

R&D Systems, part of Bio-Techne | Catalog # 11416-SE

R&D Systems, part of Bio-Techne
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11416-SE-020
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Key Product Details

Source

NS0

Accession #

P05981.1

Structure / Form

Active form

Conjugate

Unconjugated

Applications

Enzyme Activity

View all Hepsin Proteins and Enzymes »

Product Specifications

Source

Mouse myeloma cell line, NS0-derived human Hepsin protein
Arg45 to Leu417 (Asp161Glu, Arg162Lys) with a C-terminal 10-His tag
The proform was activated.

Purity

>90%, by SDS-PAGE visualized with Silver Staining and quantitative densitometry by Coomassie® Blue Staining.

Endotoxin Level

<0.10 EU per 1 μg of the protein by the LAL method.

N-terminal Sequence Analysis

Arg45 (non-catalytic chain) & Ile163 (catalytic chain)

Predicted Molecular Mass

13 kDa (non-catalytic chain), 29 kDa (catalytic chain)

SDS-PAGE

17-24 and 29-33 kDa, under reducing conditions

Activity

Measured by its ability to cleave tert-butoxycarbonyl-Gln-Arg-Arg-7-amino-4-methylcoumarin (Boc-QRR-AMC).
The specific activity is >45,000 pmol/min/μg, as measured under the described conditions.

Scientific Data Images for Recombinant Active Human Hepsin His-tag Protein, CF

Recombinant Active Human Hepsin His-tag Protein Enzyme Activity.

Recombinant Active Human Hepsin His-tag Protein (Catalog # 11416-SE) is measured by its ability to cleave tert-butoxycarbonyl-Gln-Arg-Arg-7-amino-4-methylcoumarin (Boc-QRR-AMC).

Formulation, Preparation and Storage

11416-SE
Formulation Supplied as a 0.2 μm filtered solution in Tris and NaCl.
Shipping The product is shipped with dry ice or equivalent. Upon receipt, store it immediately at the temperature recommended below.
Stability & Storage Use a manual defrost freezer and avoid repeated freeze-thaw cycles.
  • 6 months from date of receipt, -20 to -70 °C as supplied.
  • 3 months, -20 to -70 °C under sterile conditions after opening.

Background: Hepsin

Hepsin, also known as TMPRSS1, is part of a family of type II transmembrane serine proteases (TTSPs) (1) that cleaves critical target proteins including Hepatocyte growth factor (HGF), uromodulin (UMOD), uPA, and macrophage-stimulating protein (MSP) at specific cleavage sites following basic residues with a strong preference for arginine residues (2-5). Hepsin is a 417 amino acid polypeptide that is activated to a two-chain disulfide-linked form. Hepsin, like other proteases in this family, contains an N-terminal cytoplasmic tail and transmembrane domain, and an extracellular stem region with an SRCR domain and C-terminal serine protease domain with a conserved activation site (1, 6). It is most highly expressed in liver, but is also present in many other tissues, notably lung, kidney, and skeletal muscle (7) and is found at high levels in several cancers including prostate, breast, and ovarian (2, 5, 8-10). In the liver, hepsin functions to regulate glucose, lipid, and protein metabolism through proteolytic conversion of pro-HGF to HGF, a potent ligand for Met signaling and dysregulation (11). Involvement in cancers has made hepsin a target of interest using either small molecule inhibitors or antibodies to neutralize their proteolytic activity, for example for prostate cancer and metastasis (12-14). Hepsin is also of interest for its potential role in osteoarthritis (15) and its ability to cleave surface proteins of respiratory viruses making it a therapeutic target for respiratory viral diseases (13). Recombinant Human Hepsin was expressed as a secreted, soluble protein lacking its cytosolic and transmembrane domains and activated. 

References

  1. Li. S. et al. (2021) FEBS J. 288:5252.
  2. Herter, S. et al. (2005) Biochem. J. 390:125.
  3. Ganesan, R. et al. (2011) Mol. Cancer Res. 9:1175.
  4. Brunati, M. et al. (2015) Elife 4:e08887.
  5. Tanabe, L.M. and K. List (2017) FEBS J. 284:1421.
  6. Somoza, J.R. et al. (2003) Structure 11:1123.
  7. Tsuji, A. et al. (1991) J. Biol. Chem. 266:16948.
  8. Dhanasekaran, S.M. et al. (2001) Nature 412:822.
  9. Miao, J. et al. (2008) Int. J. Cancer 123:2041.
  10. Xing, P. et. al. (2011) J. Investig. Med. 59:803.
  11. Li, S. et al. (2020) Proc. Natl. Acad. Sci. USA 117:12359.
  12. Damalanka, V.C. et al. (2019) J. Med. Chem. 62:480.
  13. Murza, A. et al. (2020) Expert Opin. Ther. Pat. 30:807.
  14. Wu, Q. and Parry, G. (2007) Front. Biosci. 12:5052.
  15. Wilkinson, D.J. et al. (2017) Sci. Rep. 7:16693.

Alternate Names

HPN, TMPRSS1

Entrez Gene IDs

3249 (Human); 15451 (Mouse); 29135 (Rat)

Gene Symbol

HPN

UniProt

P05981.1

Additional Hepsin Products

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Product Specific Notices for Recombinant Active Human Hepsin His-tag Protein, CF

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