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Chemical Structure| 187034-31-7 Chemical Structure| 187034-31-7

Structure of TAPI-2
CAS No.: 187034-31-7

Chemical Structure| 187034-31-7

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TAPI-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±10 μM for MMP.

Synonyms: TNF Protease Inhibitor 2

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of TAPI-2

CAS No. :187034-31-7
Formula : C19H37N5O5
M.W : 415.53
SMILES Code : O=C(N[C@@H](C(C)(C)C)C(N[C@@H](C)C(NCCN)=O)=O)C(CC(C)C)CC(NO)=O
Synonyms :
TNF Protease Inhibitor 2
English Name :N1-((S)-1-(((S)-1-((2-Aminoethyl)amino)-1-oxopropan-2-yl)amino)-3,3-dimethyl-1-oxobutan-2-yl)-N4-hydroxy-2-isobutylsuccinamide
MDL No. :N/A

Safety of TAPI-2

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Peritoneal macrophages 2 mg/ml 1-24 hours To investigate the effect of TAPI-2 on VSIG4 release, it was found that TAPI-2 inhibited the release of VSIG4 JHEP Rep. 2021 Nov 3;4(1):100391
Human platelets 100 µM 2 hours Blocked ADAM17-mediated shedding of GPIbα and GPIX from the platelet surface Blood Adv. 2019 Dec 23;3(24):4298-4311.
Adam10/17 −/− mEFs 13.52 µM 2 hours To evaluate the inhibitory effect of TAPI-2 on ADAM9-dependent EphB4-AP shedding, results showed that TAPI-2 effectively inhibited ADAM9 activity Biochem J. 2017 Apr 13;474(9):1467-1479
C57-MKs cells 40 µM 24 hours To evaluate the effect of TAPI-2 on C57-MKs cell migration, results showed that TAPI-2 significantly inhibited CD9 downregulation-induced cell migration. Int J Biol Sci. 2019 Jan 1;15(2):493-506
HaCaT cells 40 µM 24 hours To evaluate the effect of TAPI-2 on HaCaT cell migration, results showed that TAPI-2 significantly inhibited CD9 downregulation-induced cell migration. Int J Biol Sci. 2019 Jan 1;15(2):493-506
Primary human conjunctival epithelial cells (HCECs) 10 and 100 mM 24 hours Inhibited PMA-induced sTNFR1 release and enhanced surface expression of TNFR1 Invest Ophthalmol Vis Sci. 2008 Sep;49(9):3992-8
IOBA-NHC cells 10 and 100 mM 24 hours Inhibited PMA-induced sTNFR1 release and enhanced surface expression of TNFR1 Invest Ophthalmol Vis Sci. 2008 Sep;49(9):3992-8
MDA-MB-231 cells 20 µM 24 hours Inhibited ADAM17 activity, reduced proliferation, invasion, and angiogenesis of MDA-MB-231 cells Cancer Biol Ther. 2009 Jun;8(11):1045-54
Human CD14+ monocyte-derived dendritic cells (DCs) 20 µM 2-6 hours Enhances cell surface TmTNF detection and reduces sTNF accumulation in the supernatant MAbs. 2017 May/Jun;9(4):680-695
Human CD14+ monocyte-derived macrophages 20 µM 2-6 hours Enhances cell surface TmTNF detection and reduces sTNF accumulation in the supernatant MAbs. 2017 May/Jun;9(4):680-695
Human CD14+ monocytes 20 µM 2-6 hours Enhances cell surface TmTNF detection and reduces sTNF accumulation in the supernatant MAbs. 2017 May/Jun;9(4):680-695
HuH-7 cells 200 nM 3 and 6 hours To study the effect of TAPI-2 on SARS-S protein-induced TACE activity. Results showed that TAPI-2 completely blocked the TACE activity upregulated by SARS-S protein. Antiviral Res. 2010 Mar;85(3):551-5
Vero E6 cells 200 nM 3 and 6 hours To study the effect of TAPI-2 on SARS-S protein-induced ACE2 shedding. Results showed that TAPI-2 significantly inhibited ACE2 shedding. Antiviral Res. 2010 Mar;85(3):551-5
Rat primary cortical neurons (rPCNs) 10 µM 30 min UTP-induced sAPPα release was completely inhibited J Neurochem. 2009 Jun;109(5):1300-10
Primary bronchial epithelial cells (PBECs) 2.5 µM 30 min pretreatment followed by 24-hours exposure TAPI-2 significantly inhibited IL-8 production in PBECs, indicating the involvement of TAPI-2-sensitive metalloproteinases in IL-8 regulation. Respir Res. 2011 Aug 23;12(1):110
HEK293T cells 100 and 200 nM 4 hours To study the effect of TAPI-2 on SARS-S pseudotyped virus entry. Results showed that TAPI-2 significantly attenuated viral entry. Antiviral Res. 2010 Mar;85(3):551-5
Primary ovarian cancer cells 100 µM 48 hours To evaluate the effect of ADAM-10/ADAM-17 inhibitors on CXCL16 membrane shedding and cell migration in primary ovarian cancer cells. Results showed that TAPI-2 and GI254023x treatment significantly decreased CXCL16 membrane shedding and strongly reduced cell migration of primary ovarian cancer cells. Br J Cancer. 2014 Mar 18;110(6):1535-44
A2780 cells 100 µM 48 hours To evaluate the effect of ADAM-10/ADAM-17 inhibitors on CXCL16 membrane shedding and cell migration. Results showed that TAPI-2 and GI254023x treatment significantly decreased CXCL16 membrane shedding and strongly reduced cell migration of A2780 cells. Br J Cancer. 2014 Mar 18;110(6):1535-44
Rat mesangial cells 100 µM 48 hours Inhibited high glucose-induced EGFR Tyr-845 and Tyr-1173 phosphorylation and collagen IV accumulation Diabetes. 2013 Nov;62(11):3874-86
HT29 cells 20 µM 48 hours TAPI-2 decreased the protein levels of cleaved Notch1 and HES-1 in CRC cells, reduced sphere formation and the number of ALDH+ cells Stem Cells Transl Med. 2016 Mar;5(3):331-8
HCP-1 cells 20 µM 48 hours TAPI-2 decreased the protein levels of cleaved Notch1 and HES-1 in CRC cells, reduced sphere formation and the number of ALDH+ cells Stem Cells Transl Med. 2016 Mar;5(3):331-8
Embryonic mouse hippocampal neurons 20 µM 6 hours TAPI-2 completely inhibited Aβ1–42-induced neuronal death but had no effect on staurosporine-induced death. J Neurosci. 2008 Apr 9;28(15):3941-6
HaCaT cells 40 µM 6 hours To investigate the effect of TAPI-2 on EF-induced collective directional migration of HaCaT cells. Results showed that TAPI-2 significantly reduced EF-induced directional migration and trajectory speed. J Cell Mol Med. 2020 Dec;24(23):14073-14085
MDA-MB-231 cells 5, 10, 20, 40, 80 µM 72 hours Evaluated the inhibitory effect of TAPI-2 on MDA-MB-231 cell growth, showing significant inhibition Cancer Biol Ther. 2009 Jun;8(11):1045-54
MDA-MB-231 25 µM Overnight Inhibition of TβRIII shedding through treatment with TAPI-2 rescued TβRIII mediated inhibition of BMP induced Smad1/5/8 phosphorylation Neoplasia. 2014 Jun;16(6):489-500
HMECs 25 µM Overnight Inhibition of TβRIII shedding through treatment with TAPI-2 rescued TβRIII mediated inhibition of BMP induced Smad1/5/8 phosphorylation Neoplasia. 2014 Jun;16(6):489-500

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.03mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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