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Literature summary for 3.1.3.86 extracted from

  • Thomas, M.P.; Erneux, C.; Potter, B.V.
    SHIP2 structure, function and inhibition (2017), ChemBioChem, 18, 233-247 .
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
AQX-016A
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-[(S)-hydroxy(2-phenylbenzo[h]quinolin-4-yl)methyl]piperidin-1-ium
-
Homo sapiens
(2R)-2-[(S)-[5,7-dichloro-3-adamantyl)naphthalen-1-yl](hydroxy)methyl]piperidin-1-ium
-
Homo sapiens
2-[1-[(2,4-dichlorophenyl)methyl]-2-methyl-5-(methylsulfanyl)-1H-indol-3-yl]ethan-1-aminium 40% inhibition at 0.5 mM Homo sapiens
2-[1-[(2-chlorophenyl)methyl]-2-methyl-5-(methylsulfanyl)-1H-indol-3-yl]ethan-1-aminium
-
Homo sapiens
3-[(2,4-dichlorophenyl)methoxy]-N-[(2,6-difluorophenyl)methyl]thiophene-2-carboxamide AS1938909, competitive inhibitor of SHIP2 Homo sapiens
3-[(4-chlorophenyl)methoxy]-N-[(1S)-1-phenylethyl]thiophene-2-carboxamide AS1949490, competitive inhibitor of SHIP2 Homo sapiens
benzene 1,2,3,4-tetrayl tetrakis(phosphate)
-
Homo sapiens
benzene 1,2,3,5-tetrayl tetrakis(phosphate)
-
Homo sapiens
benzene 1,2,4,5-tetrayl tetrakis(phosphate)
-
Homo sapiens
biphenyl 2,3',4,5',6-pentayl pentakis(phosphate)
-
Homo sapiens
additional information not inhibited by 3-alpha-aminocholestane Homo sapiens
N-(4-[[(4-chlorophenyl)methoxy]methyl]pyridin-2-yl)-2-phenylacetamide
-
Homo sapiens
N-(4-[[(4-chlorophenyl)methoxy]methyl]pyridin-2-yl)-3-phenylpropanamide
-
Homo sapiens
N-[4-[(4-chlorophenyl)methoxy]pyridin-2-yl]-2-(2,6-difluorophenyl)acetamide
-
Homo sapiens
N-[4-[(4-chlorophenyl)methoxy]pyridin-2-yl]-2-phenylacetamide
-
Homo sapiens
N-[4-[(4-chlorophenyl)methoxy]pyridin-2-yl]-3-phenylpropanamide
-
Homo sapiens
NGD-61338
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate + H2O Homo sapiens
-
1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate + phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens O15357
-
-

Source Tissue

Source Tissue Comment Organism Textmining
3T3-L1 cell
-
Homo sapiens
-
breast cancer cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-
K-562 cell
-
Homo sapiens
-
laryngeal squamous cell carcinoma cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-
U-251 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate + H2O
-
Homo sapiens 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate + phosphate
-
?

Synonyms

Synonyms Comment Organism
INPPL1
-
Homo sapiens
phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2
-
Homo sapiens
SHIP2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00057
-
3-[(2,4-dichlorophenyl)methoxy]-N-[(2,6-difluorophenyl)methyl]thiophene-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00062
-
3-[(4-chlorophenyl)methoxy]-N-[(1S)-1-phenylethyl]thiophene-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.03
-
(2R)-2-[(S)-hydroxy(2-phenylbenzo[h]quinolin-4-yl)methyl]piperidin-1-ium pH and temperature not specified in the publication Homo sapiens
0.063
-
(2R)-2-[(S)-[5,7-dichloro-3-adamantyl)naphthalen-1-yl](hydroxy)methyl]piperidin-1-ium pH and temperature not specified in the publication Homo sapiens
0.5
-
2-[1-[(2-chlorophenyl)methyl]-2-methyl-5-(methylsulfanyl)-1H-indol-3-yl]ethan-1-aminium pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00057
-
pH and temperature not specified in the publication Homo sapiens 3-[(2,4-dichlorophenyl)methoxy]-N-[(2,6-difluorophenyl)methyl]thiophene-2-carboxamide
0.00062
-
pH and temperature not specified in the publication Homo sapiens 3-[(4-chlorophenyl)methoxy]-N-[(1S)-1-phenylethyl]thiophene-2-carboxamide
0.03
-
pH and temperature not specified in the publication Homo sapiens (2R)-2-[(S)-hydroxy(2-phenylbenzo[h]quinolin-4-yl)methyl]piperidin-1-ium
0.063
-
pH and temperature not specified in the publication Homo sapiens (2R)-2-[(S)-[5,7-dichloro-3-adamantyl)naphthalen-1-yl](hydroxy)methyl]piperidin-1-ium
0.5
-
pH and temperature not specified in the publication Homo sapiens 2-[1-[(2-chlorophenyl)methyl]-2-methyl-5-(methylsulfanyl)-1H-indol-3-yl]ethan-1-aminium

Expression

Organism Comment Expression
Homo sapiens virusecurinine, a plant alkaloid, downregulates enzyme expression down

General Information

General Information Comment Organism
malfunction enzyme mutations are associated with opsismodysplasia. Mice expressing a germline catalytically inactive SHIP2 mutant protein are viable, but have defects in the development of muscle, adipose tissue and the female genital tract, as well as in somatic growth Homo sapiens
physiological function the enzyme is involved in insulin signalling Homo sapiens