TAPI-2 (Synonyms: TNF Protease Inhibitor 2)

Name: TAPI-2
Brand: MedChemExpress
SKU: HY-100211
Rating: 4.5 (4 reviews)

Cat. No.: HY-100211 Purity: 99.46%: FAQs
Data Sheet SDS COA Handling Instructions

TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC₅₀ of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.

For research use only. We do not sell to patients.

TAPI-2 Chemical Structure

CAS No. : 187034-31-7

Size	Price	Stock	Quantity
1 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 792	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1254	In-stock	Estimated Time of Arrival: December 31
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100 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of TAPI-2:

(R)-TAPI-2 Get quote

4 Publications Citing Use of MCE TAPI-2

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View All Isoforms

MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC₅₀ of 20 μM for MMP^[1]. TAPI-2 blocks the entry of infectious SARS-CoV^[2].

IC₅₀ & Target^[1]

MMP

20 μM (IC₅₀)

In Vitro

The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC₅₀ 20±10 μM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit. Generally, hmeprin α is inhibited more strongly than the β subunit^[1]. Without affecting ADAM17 expression, TAPI-2 dramatically decreases the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells. Moreover, treating cells with TAPI-2 significantly decreases the CSC phenotype by -50% in both CRC cell lines. The dose-dependent effects of TAPI-2 on the sphere formation and protein levels of NICD and HES-1 confirm that the concentration used (20 μM) is within the effective dose range of TAPI-2 (5-40 μM)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

415.53

Appearance

Solid

Formula

C₁₉H₃₇N₅O₅

CAS No.

187034-31-7

SMILES

CC(C)(C)[C@@H](C(N[C@H](C(NCCN)=O)C)=O)NC(C(CC(NO)=O)CC(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (240.66 mM; Need ultrasonic)

Ethanol : 50 mg/mL (120.33 mM; Need warming)

DMSO : ≥ 22 mg/mL (52.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4066 mL	12.0328 mL	24.0657 mL
5 mM	0.4813 mL	2.4066 mL	4.8131 mL
10 mM	0.2407 mL	1.2033 mL	2.4066 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 99.46%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (244 KB) HNMR (459 KB) NP-HPLC (402 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Content Brief]

[2]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [Content Brief]

[3]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [Content Brief]

Cell Assay
^[3]

TAPI-2 is dissolved in DMSO and diluted with appropriate medium before use. All experiments are performed using 20 μM TAPI-2. Cells are cultured with or without TAPI-2 for 48 hours and then seeded at 3,000 cells per well in 96-well plates. After pretreatment, increasing doses of 5-fluorouracil (5-FU) that are relevant to the recommended clinical dose (up to 2 μg/mL) are added, with or without TAPI-2, for 72 hours. Cell viability is assessed by adding MTT substrate (0.25% in phosphate-buffered saline [PBS]) in growth medium (1:5 dilution) to cells for 1 hour at 37°C. The cells are ished with PBS, and 100 μL of dimethyl sulfoxideis added. Optical density is measured at 570 nM, and relative MTT is presented as a percentage of control^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Content Brief]

[2]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [Content Brief]

[3]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [Content Brief]

TAPI-2 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

TAPI-2187034-31-7TNF Protease Inhibitor 2TAPI2TAPI 2TNF Protease Inhibitor2TNF Protease Inhibitor-2MMPSARS-CoVMatrix metalloproteinasesSARS coronavirusInhibitorinhibitorinhibit

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TAPI-2 (Synonyms: TNF Protease Inhibitor 2)

Customer Review

Other Forms of TAPI-2:

TAPI-2 Related Antibodies

4 Publications Citing Use of MCE TAPI-2

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MMP Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

TAPI-2 Related Antibodies

TAPI-2 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

Customer Review

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