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Description: ADAM-17 (TACE) and MMP inhibitor
Chemical Name: N-[(2R)-2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-methyl-L-valyl-N-(2-aminoethyl)-L-alaninamide
Purity: ≥95% (HPLC)
Biological Activity for TAPI 2
TAPI 2 is an ADAM-17 (TACE) and MMP inhibitor (Ki = 120 nM at ADAM-17). Sensitizes cancer stem cells to the lethal effects of 5-FU in vitro. Blocks shedding of TNF-α from cell membranes.
This product is typically reconstituted in water.
Technical Data for TAPI 2
| M. Wt | 415.54 |
| Formula | C19H37N5O5 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 689284-12-6 |
| PubChem ID | 10093303 |
| InChI Key | LMIQCBIEAHJAMZ-RMTCENKZSA-N |
| Smiles | ONC(C[C@@H](CC(C)C)C(N[C@@H](C(C)(C)C)C(N[C@@H](C)C(NCCN)=O)=O)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for TAPI 2
References for TAPI 2
References are publications that support the biological activity of the product.
Moss et al (2007) Fluorescent substrates for the proteinases ADAM17, ADAM10, ADAM8, and ADAM12 useful for high-throughput inhibitor screening. Anal.Biochem. 366 144 PMID: 17548045
Wang et al (2016) A disintegrin and metalloproteinase domain 17 regulates colorectal cancer stem cells and chemosensitivity via notch1 signaling. Stem Cells Transl.Med. 5 331 PMID: 26744411
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Keywords: TAPI 2, TAPI 2 supplier, TAPI2, ADAM17, metalloproteases, MMPs, metalloproteinases, inhibits, inhibitors, adams, TNFa, TNFα, converting, enzyme, TACE, ADAMs, Matrix, Metalloprotease, 6013, Tocris Bioscience
2 Citations for TAPI 2
Citations are publications that use Tocris products. Selected citations for TAPI 2 include:
Hui et al (2014) A1 adenosine receptor-stimulated exocytosis in bladder umbrella cells requires phosphorylation of ADAM17 Ser-811 and EGF receptor transactivation. Mol Biol Cell 25 3798-812 PMID: 25232008
Jian et al (2020) Dysregulated NF-κB-Dependent ICOSL Expression in Human Dendritic Cell Vaccines Impairs T-cell Responses in Patients with Melanoma. Cancer Immunol Res 8 1554-1567 PMID: 33051240
Do you know of a great paper that uses TAPI 2 from Tocris? Please let us know.
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