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Literature summary for 3.4.22.59 extracted from

  • Heise, C.E.; Murray, J.; Augustyn, K.E.; Bravo, B.; Chugha, P.; Cohen, F.; Giannetti, A.M.; Gibbons, P.; Hannoush, R.N.; Hearn, B.R.; Jaishankar, P.; Ly, C.Q.; Shah, K.; Stanger, K.; Steffek, M.; Tang, Y.; Zhao, X.; Lewcock, J.W.; Renslo, A.R.; Flygare, J.; Arkin, M.R.
    Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6 (2012), PLoS ONE, 7, e50864.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with benzyloxycarbonyl-VEID, using 12% (w/v) PEG 3350, 0.2 M sodium malonate pH 4.0 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-[(2R)-1-(3-cyanophenyl)-3-hydroxypropan-2-yl]-5-(3,4-dimethoxyphenyl)furan-3-carboxamide selective inhibitor Homo sapiens
N-[[5-(3,4-dimethoxyphenyl)-2-methylfuran-3-yl]carbonyl]phenylalanine
-
Homo sapiens
VEID-CHO
-
Homo sapiens
VEID-fluoromethylketone
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.08
-
(N-acetyl-VEID)2-rhodamine110 in 50 mM HEPES (pH 7.0), 25 mM MgSO4, 0.5 mM EGTA, 5 mM glutathione, 0.01% (v/v) Triton X-100 containing 0.1% (w/v) bovine gamma-globulin, at 22°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P55212
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(N-acetyl-VEID)2-rhodamine110 + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Casp6
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
in 50 mM HEPES (pH 7.0), 25 mM MgSO4, 0.5 mM EGTA, 5 mM glutathione, 0.01% (v/v) Triton X-100 containing 0.1% (w/v) bovine gamma-globulin, at 22°C Homo sapiens N-[(2R)-1-(3-cyanophenyl)-3-hydroxypropan-2-yl]-5-(3,4-dimethoxyphenyl)furan-3-carboxamide
0.02
-
in 50 mM HEPES (pH 7.0), 25 mM MgSO4, 0.5 mM EGTA, 5 mM glutathione, 0.01% (v/v) Triton X-100 containing 0.1% (w/v) bovine gamma-globulin, at 22°C Homo sapiens N-[[5-(3,4-dimethoxyphenyl)-2-methylfuran-3-yl]carbonyl]phenylalanine