Reaction Details |
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Target | Disintegrin and metalloproteinase domain-containing protein 17 |
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Ligand | BDBM23498 |
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Substrate/Competitor | pro-TNF-alpha peptide |
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Meas. Tech. | TACE Inhibition Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 8.4±n/a nM |
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Citation | Zhang, Y; Xu, J; Levin, J; Hegen, M; Li, G; Robertshaw, H; Brennan, F; Cummons, T; Clarke, D; Vansell, N; Nickerson-Nutter, C; Barone, D; Mohler, K; Black, R; Skotnicki, J; Gibbons, J; Feldmann, M; Frost, P; Larsen, G; Lin, LL Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J Pharmacol Exp Ther309:348-55 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Disintegrin and metalloproteinase domain-containing protein 17 |
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Name: | Disintegrin and metalloproteinase domain-containing protein 17 |
Synonyms: | ADA17_HUMAN | ADAM17 | CSVP | Disintegrin and metalloproteinase domain-containing protein 17 (ADAM-17) | Disintegrin and metalloproteinase domain-containing protein 17 (ADAM17) | TACE | TNF-alpha convertase | TNF-alpha converting enzyme (TACE) | TNF-alpha-converting enzyme (TACE) | Tumor Necrosis Factor Alpha Converting Enzyme | Tumor necrosis factor-α converting enzyme (TACE) |
Type: | Enzyme |
Mol. Mass.: | 93007.89 |
Organism: | Homo sapiens (Human) |
Description: | |
Residue: | 824 |
Sequence: | MRQSLLFLTSVVPFVLAPRPPDDPGFGPHQRLEKLDSLLSDYDILSLSNIQQHSVRKRDL
QTSTHVETLLTFSALKRHFKLYLTSSTERFSQNFKVVVVDGKNESEYTVKWQDFFTGHVV
GEPDSRVLAHIRDDDVIIRINTDGAEYNIEPLWRFVNDTKDKRMLVYKSEDIKNVSRLQS
PKVCGYLKVDNEELLPKGLVDREPPEELVHRVKRRADPDPMKNTCKLLVVADHRFYRYMG
RGEESTTTNYLIELIDRVDDIYRNTSWDNAGFKGYGIQIEQIRILKSPQEVKPGEKHYNM
AKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANS
HGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGL
AECAPNEDQGGKYVMYPIAVSGDHENNKMFSNCSKQSIYKTIESKAQECFQERSNKVCGN
SRVDEGEECDPGIMYLNNDTCCNSDCTLKEGVQCSDRNSPCCKNCQFETAQKKCQEAINA
TCKGVSYCTGNSSECPPPGNAEDDTVCLDLGKCKDGKCIPFCEREQQLESCACNETDNSC
KVCCRDLSGRCVPYVDAEQKNLFLRKGKPCTVGFCDMNGKCEKRVQDVIERFWDFIDQLS
INTFGKFLADNIVGSVLVFSLIFWIPFSILVHCVDKKLDKQYESLSLFHPSNVEMLSSMD
SASVRIIKPFPAPQTPGRLQPAPVIPSAPAAPKLDHQRMDTIQEDPSTDSHMDEDGFEKD
PFPNSSTAAKSFEDLTDHPVTRSEKAASFKLQRQNRVDSKETEC
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BDBM23498 |
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pro-TNF-alpha peptide |
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Name: | pro-TNF-alpha peptide |
Synonyms: | n/a |
Type: | Fluorogenic peptide |
Mol. Mass.: | 1429.56 |
Organism: | n/a |
Description: | A proprietary synthetic peptide of pro-TNF-alpha containing the minimal TACE cleavage sequence. |
Residue: | 14 |
Sequence: | |