Recombinant Human Transmembrane protease serine 2 (TMPRSS2), partial (Active)

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文獻引用 (12)

中文名稱：

人TMPRSS2重組蛋白
貨號：

CSB-YP023924HU
說明書：

MSDS Datasheet
規(guī)格：

￥1836
圖片：
(Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.

Recombinant Human TMPRSS2 His tag protein (CSB-YP023924HU) enzyme activity is measured by its ability to cleave fluorogenic peptide substrate(Boc-Gln-Ala-Arg-AMC), The Km is 21.93μM. Biological Activity Assay

Activity
Measured by Camostat Mesylate inhibit ratio on TMPRSS2 (CSB-YP023924HU), which can cleave fluorogenic peptide substrate (Boc-Gln-Ala-Arg-AMC). The Camostat Mesylate inhibit EC₅₀ is 0.03347-0.07945μM. Biological Activity Assay
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產品評價
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靶點詳情

產品詳情

純度：

Greater than 85% as determined by SDS-PAGE.
生物活性：

①Recombinant Human TMPRSS2 His tag protein (CSB-YP023924HU) enzyme activity is measured by its ability to cleave fluorogenic peptide substrate(Boc-Gln-Ala-Arg-AMC), The Km is 21.93μM. ②Measured by Camostat Mesylate inhibit ratio on TMPRSS2 (CSB-YP023924HU), which can cleave fluorogenic peptide substrate (Boc-Gln-Ala-Arg-AMC). The Camostat Mesylate inhibit EC50 is 0.03347-0.07945μM.
基因名：

TMPRSS2
Uniprot No.：

O15393
別名：

TMPRSS2; PRSS10; Transmembrane protease serine 2; Serine protease 10
種屬：

Homo sapiens (Human)
蛋白長度：

Partial
來源：

Yeast
分子量：

44.8kDa
表達區(qū)域：

106-492 aa
氨基酸序列

WKFMGSKCSNSGIECDSSGTCINPSNWCDGVSHCPGGEDENRCVRLYGPNFILQVYSSQRKSWHPVCQDDWNENYGRAACRDMGYKNNFYSSQGIVDDSGSTSFMKLNTSAGNVDIYKKLYHSDACSSKAVVSLRCIACGVNLNSSRQSRIVGGESALPGAWPWQVSLHVQNVHVCGGSIITPEWIVTAAHCVEKPLNNPWHWTAFAGILRQSFMFYGAGYQVEKVISHPNYDSKTKNNDIALMKLQKPLTFNDLVKPVCLPNPGMMLQPEQLCWISGWGATEEKGKTSEVLNAAKVLLIETQRCNSRYVYDNLITPAMICAGFLQGNVDSCQGDSGGPLVTSKNNIWWLIGDTSWGSGCAKAYRPGVYGNVMVFTDWIYRQMRADG
蛋白標簽：

N-terminal 6xHis-tagged
產品提供形式：

Liquid or Lyophilized powder Warning: in_array() expects parameter 2 to be array, null given in /www/web/cusabio_cn/public_html/caches/caches_template/default/content/show_product_protein.php on line 662
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
緩沖液：

If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.
Note: If you have any special requirement for the glycerol content, please remark when you place the order.
If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose.
復溶：

We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.
儲存條件：

Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
保質期：

The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
貨期：

3-7 business days
注意事項：

Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
產品描述：

The recombinant active human Transmembrane protease serine 2 (TMPRSS2) is produced by the expression of a target DNA sequence with 6xHis, N-terminal tag(s), in the yeast expression system. The target DNA sequence encodes the 106-492aa region of the human TMPRSS2. The purity of this partial-length protein is greater than 85% determined by SDS-PAGE. The gel showed a molecular weight band of about 45 kDa under reducing conditions. And its enzymatic activity was verified by its ability to cleave fluorogenic peptide substrate (Boc-Gln-Ala-Arg-AMC) (Km is 21.93μM).

The protease TMPRSS2 plays an important role in the infection mechanism of human coronaviruses, such as SARS-CoV and SARS-CoV-2. Cell entry of human coronaviruses depends on the binding of the viral spike (S) glycoprotein to cellular ACE2 receptor and S protein priming by host cell protease TMPRSS2. Moreover, TMPRSS2 protein is commonly used to study cancer. Previous studies have shown that the TMPRSS2 gene was up-regulated by androgenic hormones in prostate cancer cells and down-regulated in androgen-independent prostate cancer tissue.
Datasheet & COA：

Please contact us to get it.

引用文獻

From N-0385 to N-0920: Unveiling a Host-Directed Protease Inhibitor with Picomolar Antiviral Efficacy against Prevalent SARS-CoV-2 Variants G Lemieux, J Pérez-Vargas, A Désilets,Journal of Medicinal Chemistry,2025
Notes on AEMS methods development for high throughput experimentation in drug discovery M Verma, N Hoxie, J Janiszewski, C Bonney, MD Hall,SLAS technology,2024
The Proteolytic Activity of Neutrophil-Derived Serine Proteases Bound to the Cell Surface Arming Lung Epithelial Cells for Viral Defense A Assylbekova, M Allayarova, M Konysbekova,Molecules,2024
Small molecule in situ resin capture provides a compound first approach to natural product discovery A Bogdanov,nature communications,2024
In vitro testing of host-targeting small molecule antiviral matriptase/TMPRSS2 inhibitors in 2D and 3D cell-based assays N van Eijk,Biomedicine & pharmacotherapy,2023
Optimization of Ketobenzothiazole‐Based Type II Transmembrane Serine Protease Inhibitors to Block H1N1 Influenza Virus Replication é Colombo,ChemMedChem,2024
Discovery of Triple Inhibitors of Both SARS-CoV-2 Proteases and Human Cathepsin L Ittipat Meewan,Pharmaceuticals,2022
Novel cleavage sites identified in SARS-CoV-2 spike protein reveal mechanism for cathepsin L-facilitated viral infection and treatment strategies MM Zhao,Cell discovery,2022
Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors O Pilgram,European Journal of Medicinal Chemistry,2022
Serine Protease Inhibitors Restrict Host Susceptibility to SARS-CoV-2 Infections E Rosendal,mBio,2022
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L Anneliese S Ashhurst,Journal of medicinal chemistry,2021
Antiviral Potential of the Antimicrobial Drug Atovaquone against SARS-CoV-2 and Emerging Variants of Concern ME Carter-Timofte,ACS infectious diseases,2021

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產品評價

問答及客戶評論

■ 常見問題解答

What QC test will you perform?

Quality Control:
1. Cloning Stage: Sequencing of the expression plasmid to ensure that the gene is completely correct. (Free of Charge. It is our routine detection.)
2. Protein Stage:
2.1. SDS-PAGE detection to determine purity and molecular weight (determine whether the observed value and the theoretical value are consistent). We comprehensively evaluate the purity through SDS-PAGE Coomassie brilliant blue staining detection and analysis using Bandscan software to ensure that the purity is more than 90%. (Free of Charge. It is our routine detection.)
2.2. Each batch will be tested for activity before shipped. (Free of Charge. It is our routine detection.)
2.3. WB detection (It is generally WB detection of tag-antibody, if there is a corresponding specific antibody, it will be arranged) to further determine the molecular weight of the protein (determine whether the observed value and the theoretical value are consistent) and its specificity. (Free of Charge. It will be performed upon customers' requests.)
2.4. AKTA-SEC test: For customers who need it, it can be used as a molecular sieve for further purification, while determining the purity and morphology of the protein (judging the presence of multimers). (Paid Service. It will be performed upon customers' requests.)
2.5. MS Identification: For customers who need it, we can arrange for mass spectrometry identification a separate sample. (Paid Service. It will be performed upon customers' requests.)
2.6. MS Identification: There is also a free monthly mass spectrometry identification (mixed samples will be detected). (Free of Charge. It is our routine detection.)

What is the general protectant? What kind of protectant do you usually add?

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

When making TMPRSS2, do you use any protein denaturing purification steps?

No, we don't use any protein denaturing purification steps. The protein is purified under mild conditions to avoid denaturation of the protein and to preserve the protein's natural state to the maximum.

Is TMPRSS2 soluble in water (buffer) or is it necessary to resuspend products in a solvent such as DMSO?

It's soluble in Tris-buffer.

Was it difficult to manufacture TMPRSS2?

The expression of TMPRSS2 is not difficult. We've expressed it successfully and have stable stock of it.

Do you know whether this product has been tested for activity?

We're conducting activity testing for this protein. The activity data will be uploaded once the testing is finished.

I want to order 500 μg of CSB-YP023924HU. Would you let me know what form of the protein is provided (liquid or powder)?

The default shipping form is lyophilized powder. If you want liquid form, we can also meet, please note when ordering.

Can you remove the endotoxin?

Yes. We can provide endotoxin removal service free of charge and guarantee the endotoxin level to be less than 0.1ng/μg (1EU μg).

What is the general preservative? Which kind of preservative do you usually add?

Commonly used preservative include Proclin 300, Sodium azide, etc. We do not add any preservative to our protein.

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靶點詳情

功能：

Plasma membrane-anchored serine protease that participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia.; (Microbial infection) Facilitates human coronaviruses SARS-CoV and SARS-CoV-2 infections via two independent mechanisms, proteolytic cleavage of ACE2 receptor which promotes viral uptake, and cleavage of coronavirus spike glycoproteins which activates the glycoprotein for host cell entry. Upon SARS-CoV-2 infection, increases syncytia formation by accelerating the fusion process. Proteolytically cleaves and activates the spike glycoproteins of human coronavirus 229E (HCoV-229E) and human coronavirus EMC (HCoV-EMC) and the fusion glycoproteins F0 of Sendai virus (SeV), human metapneumovirus (HMPV), human parainfluenza 1, 2, 3, 4a and 4b viruses (HPIV). Essential for spread and pathogenesis of influenza A virus (strains H1N1, H3N2 and H7N9); involved in proteolytic cleavage and activation of hemagglutinin (HA) protein which is essential for viral infectivity.
基因功能參考文獻：
1. A potential novel function of TMPRSS2-ERG as a major regulator of IGF1R gene expression. PMID: 27285981
2. Study shows that T2E fusion transcripts are associated with higher levels of AMACR mRNA in patients with atypical small acinar proliferation (ASAP) which represents an indicator of risk for prostate cancer in patients with ASAP. PMID: 29277318
3. TMPRSS2-ERG may have a role in progression of prostate neoplasms and in alteration of the metabolic profile PMID: 27276682
4. We propose that epigenetic events are a significant and alternative driver of aggressive disease in TMPRSS2-ERG fusion-negative prostate cancer. PMID: 27814612
5. Meta-analysis showed the prevalence of TMPRSS2:ERG fusions in prostate cancer to be highest in men of European descent (49%), followed by Asians (27%) and then African (25%) descent. PMID: 28633309
6. Data show that tumors displaying TMPRSS2-ERG fusions that retained interstitial genes were less likely to be associated with biochemical recurrence PMID: 29127096
7. We demonstrate a role for inflammation-induced oxidative stress in the formation of DNA breaks leading to recurrent TMPRSS2-ERG gene fusions. The transcriptional status and epigenetic features of the target genes influence this effect. PMID: 27926866
8. NOTCH pathway inhibition antagonizes the growth and invasion of transmembrane protease serine 2 (TMPRSS2)-transforming protein ERG (ERG) (T2E) -positive prostate cancer cells. PMID: 28783165
9. The TMPRSS2-ERG gene fusion is the most frequently observed genetic aberration in prostate cancer. PMID: 28845585
10. Study provide evidence that PTEN deletion and TMPRSS2-ERG gene fusion were mutually exclusive in patients with prostate neoplasm. TMPRSS2-ERG gene fusion was rare compared to peripheral zone tumors and to PTEN inactivation in T1a transition zone tumors. PMID: 27500376
11. miR-204 upregulates androgen receptor (AR ) and downregulates TMPRSS2/ERG through direct regulation of their promoter methylation and set of transcription factors during AR cancer-related reprogramming. PMID: 28050800
12. differential expression of TMPRSS2:ERG in urine exosomes in prostate cancer and controls PMID: 27144529
13. The present study established evidence for the first two common PrCa risk variants differentially associated with TMPRSS2:ERG fusion status. TMPRSS2:ERG phenotyping of larger studies is required to determine comprehensive sets of variants with subtype-specific roles in prostate cancer. PMID: 27798103
14. Human coronavirus 229E presumably evolved to bypass the endosome by entering the cell via TMPRSS2. PMID: 27733646
15. Studies indicate that TMPRSS2-ERG fusion gene positive prostate cancers cells rewire intracellular signaling cascades and modulate gene and protein network. PMID: 28364793
16. TMPRSS2-ERG role in prostate cancer invasiveness and regulation of MMP-9 and plexin B1. PMID: 28004109
17. Our results indicate that it is possible to predict pT3 stage at final histology from TMPRSS2:ERG gene fusion at initial core needle biopsy. FISH determination of TMPRSS2:ERG gene fusion may be particularly useful for patients scheduled to undergo a radical prostatectomy in order to improve oncological and functional results PMID: 27377958
18. Data show there was a good agreement of transcriptional regulator ERG protein (ERG) immunostaining with the presence of TMPRSS2:ERG fusion protein. PMID: 27320318
19. A combination of high preoperative serum PSA and high expression of TMPRSS2-ERG could be promising in distinguishing those tumors that are aggressive and life-threatening. PMID: 27630329
20. Studies showed that urinary TMPRSS2:ERG transcripts seem to be indicative of Prostate cancer aggressiveness upon biopsy. [review] PMID: 26774207
21. Aspirin was associated with a significant reduction in the relative risk of TMPRSS2:ERG (T2E )fusion positive, but not T2E negative PMID: 26503111
22. the type II transmembrane serine protease TMPRSS2 was able to activate hemagglutinin for cell entry indicating that bat influenza A virus can utilize human proteases for hemagglutinin activation. PMID: 27028521
23. The relatively low rate of ERG-positive prostatic intraepithelial neoplasia counts in favor of the limited role of chimeric transcript TMPRSS2/ERG in the differential diagnosis of prostatic intraepithelial neoplasia PMID: 26978019
24. TMPRSS2 isoform 1 is expressed in viral target cells. PMID: 26379044
25. The TMPRSS2-ERG Gene Fusion Blocks XRCC4-Mediated Nonhomologous End-Joining Repair and Radiosensitizes Prostate Cancer Cells to PARP Inhibition PMID: 26026052
26. The potential for TMPRSS2:ERG gene fusion, detected by IHC, to modify the role of PTEN loss in lethal progression of prostate cancer. PMID: 26615022
27. Results indicate that PTEN loss occurs in cooperation with TMPRSS2-ERG fusion in prostate cancer and the majority of the samples harbor TMPRSS2-ERG fusion as well as PTEN gene deletion. PMID: 26424596
28. Elucidation of ERG regulation of ABEs in castration-resistant prostate cancer (CRPC) may help to stratify TMPRSS2-ERG fusion-positive prostate cancer patients in the clinic for anti-androgen receptor-driven therapies. PMID: 25754347
29. these data show that the androgen-driven events causing TMPRSS2-ERG fusions and other rearrangements of androgen-dependent genes in prostate epithelial cells of young patients preferentially lead to low-grade (and not high-grade) prostate cancer. PMID: 25015038
30. TMPRSS2-ERG fusion gene transcript was found in 63, 55 and 73% of the prostate cancer cases on urine alone, biopsy rinse material alone and paired samples, respectively. PMID: 24997128
31. Genetic inhibition of TMPRSS2-ERG junction oncogene in prostate cancer by means of siRNA has strong antineoplastic effect in a mouse model and in vitro. PMID: 25933120
32. Data showed that TMPRSS2 expression is not only dramatically increased in the primary cancers of patients but TMPRSS2 immunopositivity is also directly correlated with cancer pain severity in these patients. PMID: 25734995
33. High AR gene copy number emerges during the development of Small cell carcinoma of the prostate, often in association with TMPRSS2-ERG rearrangement. PMID: 24777847
34. Both IHC and qRT-PCR are useful tools in detecting TMPRSS2:ERG fusions. PMID: 25007891
35. Membrane bound meprin Beta is activated by transmembrane serine protease matriptase-2 at the cell surface. PMID: 26251449
36. Data indicate that inhibition of transcriptional regulator ERG protein expression in transmembrane protease serine 2 protein (TMPRSS2):ERG-positive prostate cancer cells increased neuroendocrine cell gene expression. PMID: 25263440
37. TMPRSS2 promotes the growth, invasion, and metastasis of prostate cancer cells via matriptase activation and extracellular matrix disruption. PMID: 26018085
38. Analysis of prostate cancer tissues showed that the presence of a TMPRSS2-ERG rearrangement was highly correlated with lower levels of NKX3.1 expression consistent with the role of NKX3.1 as a suppressor of the pathogenic gene rearrangement. PMID: 25977336
39. The TMPRSS2 Met160Val polymorphism is a genetic risk factor for sporadic prostate cancer in a Japanese population. PMID: 25040002
40. The expression levels of the TMPRSS2-ERG fusion is related to a more aggressive phenotype, have an effect on prognosis and could be molecular markers of progression for prostate cancer. PMID: 25939480
41. Results provide suggestive evidence that men with TMPRSS2:ERG positive tumors may have longer prostate cancer survival after ADT. PMID: 25728532
42. recent and maximum BMI are inversely associated with the odds of developing T2E-positive prostate cancer, but no associations were observed for T2E-negative prostate canc PMID: 25852077
43. TMPRSS2-ERG gene fusions induce prostate tumorigenesis by modulating microRNA miR-200c. PMID: 24186205
44. activates hepatitis C virus infection at the postbinding and entry stage PMID: 25203900
45. results demonstrate the ability of confocal microscopy and FISH to identify the cell-to-cell differences in common gene fusions such as TMPRSS2-ERG that may arise independently within the same tumor focus PMID: 25175909
46. The effect of TMPRSS2/ERG gene fusions had differing effects on radiosensitivity and chemosensitivity depending on cell line and fusion type. PMID: 21394739
47. These findings indicate that TMPRSS2-ERG may or may not lead to prostate cancer development PMID: 24961351
48. Report prognostic value of tissue/urinary TMPRSS2-ERG levels in prostate neoplasms. PMID: 24072184
49. concurrent in situ detection of gene expression, point mutations, and gene fusions of the prostate cancer relevant targets TMPRSS2-ERG PMID: 24931216
50. TMPRSS2:ERG gene fusion synergizes with the VDR to induce CYP24A1 expression-limiting VDR signaling. PMID: 24926821
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亞細胞定位：

Cell membrane; Single-pass type II membrane protein.; [Transmembrane protease serine 2 catalytic chain]: Secreted.
蛋白家族：

Peptidase S1 family
組織特異性：

Expressed in several tissues that comprise large populations of epithelial cells with the highest level of transcripts measured in the prostate gland. Expressed in type II pneumocytes in the lung (at protein level). Expressed strongly in small intestine.
數(shù)據庫鏈接：

HGNC: 11876

OMIM: 602060

KEGG: hsa:7113

STRING: 9606.ENSP00000381588

UniGene: Hs.439309