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Literature summary for 3.4.22.59 extracted from

  • Chu, W.; Rothfuss, J.; Chu, Y.; Zhou, D.; Mach, R.H.
    Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6 (2009), J. Med. Chem., 52, 2188-2191.
    View publication on PubMed
Search for more literature for 3.4.22.59

Inhibitors

Inhibitors Comment Organism Structure
1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione slight inhibition Homo sapiens
1-benzyl-5-(thiomorpholin-4-ylsulfonyl)-1H-indole-2,3-dione
-
 Homo sapiens
5-(azetidin-1-ylsulfonyl)-1-benzyl-1H-indole-2,3-dione
-
 Homo sapiens
5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione slight inhibition Homo sapiens
Ac-Val-Glu-Ile-Asp-CHO
-
 Homo sapiens
additional information development and synthesis of nonpeptidic caspase-6 inhibitors, overview. No inhibition of caspase-6 by Ac-IETD-CHO, Ac-YVAD-CHO, and Ac-DEVD-CHO Homo sapiens
sulfonamide isatin Michael acceptors small molecule inhibitors of caspase-6 Homo sapiens
[1-(3,4-dichlorobenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(3,4-dichlorobenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(3,4-dichlorobenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(4-methoxybenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(4-methoxybenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(4-methoxybenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-(4-methoxybenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-benzyl-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-benzyl-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-benzyl-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[1-benzyl-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[5-(azetidin-1-ylsulfonyl)-1-(3,4-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[5-(azetidin-1-ylsulfonyl)-1-(4-methoxybenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens
[5-(azetidin-1-ylsulfonyl)-1-benzyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
huntingtin + H2O Homo sapiens a key step in the onset of Huntington’s disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments huntingtin peptide fragments
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
huntingtin + H2O
-
 Homo sapiens huntingtin peptide fragments
-
 ?
huntingtin + H2O a key step in the onset of Huntington’s disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments Homo sapiens huntingtin peptide fragments
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000151
-
-
 Homo sapiens [1-benzyl-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000156
-
-
 Homo sapiens [5-(azetidin-1-ylsulfonyl)-1-benzyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000188
-
-
 Homo sapiens [1-(4-methoxybenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000197
-
-
 Homo sapiens [5-(azetidin-1-ylsulfonyl)-1-(4-methoxybenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.00023
-
-
 Homo sapiens [1-(3,4-dichlorobenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000241
-
-
 Homo sapiens [1-benzyl-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.00028
-
-
 Homo sapiens [5-(azetidin-1-ylsulfonyl)-1-(3,4-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000325
-
-
 Homo sapiens [1-benzyl-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000358
-
-
 Homo sapiens [1-(4-methoxybenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000425
-
-
 Homo sapiens [1-benzyl-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000453
-
-
 Homo sapiens [1-(4-methoxybenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000468
-
-
 Homo sapiens [1-(3,4-dichlorobenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000545
-
-
 Homo sapiens [1-(4-methoxybenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000568
-
-
 Homo sapiens [1-(3,4-dichlorobenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.000592
-
-
 Homo sapiens [1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile
0.00128
-
-
 Homo sapiens 1-benzyl-5-(thiomorpholin-4-ylsulfonyl)-1H-indole-2,3-dione
0.0015
-
 above Homo sapiens 1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione
0.002
-
 above Homo sapiens 5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione
0.00983
-
-
 Homo sapiens 5-(azetidin-1-ylsulfonyl)-1-benzyl-1H-indole-2,3-dione