Reaction Details |
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Target | Caspase-8 |
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Ligand | BDBM10539 |
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Substrate/Competitor | Caspase-8 Fluorogenic Substrate |
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Meas. Tech. | Caspase Inhibition Assay |
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IC50 | 7270±n/a nM |
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Citation | Mellon, C; Aspiotis, R; Black, CW; Bayly, CI; Grimm, EL; Giroux, A; Han, Y; Isabel, E; McKay, DJ; Nicholson, DW; Rasper, DM; Roy, S; Tam, J; Thornberry, NA; Vaillancourt, JP; Xanthoudakis, S; Zamboni, R Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors. Bioorg Med Chem Lett15:3886-90 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Caspase-8 |
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Name: | Caspase-8 |
Synonyms: | Apoptotic cysteine protease | Apoptotic protease Mch-5 | CAP4 | CASP-8 | CASP8 | CASP8_HUMAN | Caspase | Caspase-8 subunit p10 | Caspase-8 subunit p18 | FADD-homologous ICE/CED-3-like protease | FADD-like ICE | FLICE | ICE-like apoptotic protease 5 | MACH | MCH5 | MORT1-associated CED-3 homolog |
Type: | Enzyme |
Mol. Mass.: | 55373.89 |
Organism: | Homo sapiens (Human) |
Description: | Q14790 |
Residue: | 479 |
Sequence: | MDFSRNLYDIGEQLDSEDLASLKFLSLDYIPQRKQEPIKDALMLFQRLQEKRMLEESNLS
FLKELLFRINRLDLLITYLNTRKEEMERELQTPGRAQISAYRVMLYQISEEVSRSELRSF
KFLLQEEISKCKLDDDMNLLDIFIEMEKRVILGEGKLDILKRVCAQINKSLLKIINDYEE
FSKERSSSLEGSPDEFSNGEELCGVMTISDSPREQDSESQTLDKVYQMKSKPRGYCLIIN
NHNFAKAREKVPKLHSIRDRNGTHLDAGALTTTFEELHFEIKPHDDCTVEQIYEILKIYQ
LMDHSNMDCFICCILSHGDKGIIYGTDGQEAPIYELTSQFTGLKCPSLAGKPKVFFIQAC
QGDNYQKGIPVETDSEEQPYLEMDLSSPQTRYIPDEADFLLGMATVNNCVSYRNPAEGTW
YIQSLCQSLRERCPRGDDILTILTEVNYEVSNKDDKKNMGKQMPQPTFTLRKKLVFPSD
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BDBM10539 |
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Caspase-8 Fluorogenic Substrate |
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Name: | Caspase-8 Fluorogenic Substrate |
Synonyms: | Ac-IETD-AMC |
Type: | Peptide |
Mol. Mass.: | 1673.49 |
Organism: | n/a |
Description: | AMC=7-Amino-4-methylcoumarin |
Residue: | 16 |
Sequence: | |