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Target
Caspase-8
Ligand
BDBM10220
Substrate
Caspase-8 Fluorogenic Substrate
Meas. Tech.
Enzyme Inhibition Assay
IC50
75000±n/a nM
Citation
 Fattorusso, R; Jung, D; Crowell, KJ; Forino, M; Pellecchia, M Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach. J Med Chem 48:1649-56 (2005) [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:
BDBM10220
Synonyms:
2-(2,3-dihydro-1,4-benzodioxin-2-yl)-1,3-thiazole-4-carboxylic acid | BI-9C1 | Burnham Institute Compound 6
Type:
Small organic molecule
Emp. Form.:
C12H9NO4S
Mol. Mass.:
263.269
SMILES:
OC(=O)c1csc(n1)C1COc2ccccc2O1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Caspase-8 Fluorogenic Substrate
Synonyms:
n/a
Type:
n/a
Mol. Mass.:
1689.47
Organism:
n/a
Description:
AFC=7-Amino-4-trifluoromethylcoumarin
Residue:
16
Sequence:
ACILEGLTHRASPAFC