Reaction Details |
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Target | Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
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Ligand | BDBM26558 |
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Substrate/Competitor | TACE Substrate Peptide |
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Meas. Tech. | TACE Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 30±n/a nM |
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Citation | Bandarage, UK; Wang, T; Come, JH; Perola, E; Wei, Y; Rao, BG Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones. Bioorg Med Chem Lett18:44-8 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
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Name: | Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
Synonyms: | A disintegrin and metalloproteinase domain 17 | ADA17_HUMAN | ADAM 17 | ADAM17 | CD156b antigen | CSVP | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme |
Type: | Single-pass type I membrane protein; metalloprotease |
Mol. Mass.: | 29695.98 |
Organism: | Homo sapiens (Human) |
Description: | The catalytic domain of recombinant human TNF-converting enzyme (residues 215-477) with two mutations (S266A and N452Q) and a 6xHis was purified from the baculovirus/Hi5 cells expression system. |
Residue: | 263 |
Sequence: | RADPDPMKNTCKLLVVADHRFYRYMGRGEESTTTNYLIELIDRVDDIYRNTAWDNAGFKG
YGIQIEQIRILKSPQEVKPGEKHYNMAKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCL
AHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTI
LTKEADLVTTHELGHNFGAEHDPDGLAECAPNEDQGGKYVMYPIAVSGDHENNKMFSQCS
KQSIYKTIESKAQECFQERSNKV
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BDBM26558 |
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TACE Substrate Peptide |
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Name: | TACE Substrate Peptide |
Synonyms: | Bachem M-2155 | DABCYL-TNF-alpha-EDANS (-4 to +6) (human) |
Type: | Internally quenched peptide |
Mol. Mass.: | 4104.44 |
Organism: | n/a |
Description: | n/a |
Residue: | 39 |
Sequence: | DABCYL-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Arg-EDANS
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