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Target
Caspase-8
Ligand
BDBM10661
Substrate
Caspase-8 Fluorogenic Substrate
Meas. Tech.
Caspase Inhibition Assay
IC50
3300±n/a nM
Citation
 Han, Y; Giroux, A; Grimm, EL; Aspiotis, R; Francoeur, S; Bayly, CI; Mckay, DJ; Roy, S; Xanthoudakis, S; Vaillancourt, JP; Rasper, DM; Tam, J; Tawa, P; Thornberry, NA; Paterson, EP; Garcia-Calvo, M; Becker, JW; Rotonda, J; Nicholson, DW; Zamboni, RJ Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors. Bioorg Med Chem Lett 14:805-8 (2004) [PubMed]  Article 
Target
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:
MDFSRNLYDIGEQLDSEDLASLKFLSLDYIPQRKQEPIKDALMLFQRLQEKRMLEESNLSFLKELLFRINRLDLLITYLNTRKEEMERELQTPGRAQISAYRVMLYQISEEVSRSELRSFKFLLQEEISKCKLDDDMNLLDIFIEMEKRVILGEGKLDILKRVCAQINKSLLKIINDYEEFSKERSSSLEGSPDEFSNGEELCGVMTISDSPREQDSESQTLDKVYQMKSKPRGYCLIINNHNFAKAREKVPKLHSIRDRNGTHLDAGALTTTFEELHFEIKPHDDCTVEQIYEILKIYQLMDHSNMDCFICCILSHGDKGIIYGTDGQEAPIYELTSQFTGLKCPSLAGKPKVFFIQACQGDNYQKGIPVETDSEEQPYLEMDLSSPQTRYIPDEADFLLGMATVNNCVSYRNPAEGTWYIQSLCQSLRERCPRGDDILTILTEVNYEVSNKDDKKNMGKQMPQPTFTLRKKLVFPSD
  
Inhibitor
Name:
BDBM10661
Synonyms:
(3S)-5-(benzylsulfanyl)-3-[(2S)-2-[(5-fluoro-1H-indol-2-yl)formamido]-3-methylbutanamido]-4-oxopentanoic acid | valine aspartyl ketone analog 3
Type:
Small organic molecule
Emp. Form.:
C26H28FN3O5S
Mol. Mass.:
513.581
SMILES:
CC(C)[C@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)N[C@@H](CC(O)=O)C(=O)CSCc1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
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:
ACILEGLTHRASPAMC