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Literature summary for 2.3.1.50 extracted from

  • Adachi, R.; Asano, Y.; Ogawa, K.; Oonishi, M.; Tanaka, Y.; Kawamoto, T.
    Pharmacological characterization of synthetic serine palmitoyltransferase inhibitors by biochemical and cellular analyses (2018), Biochem. Biophys. Res. Commun., 497, 1171-1176 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-chloro-N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]benzamide
-
Homo sapiens
myriocin
-
Homo sapiens
N-[(7S)-4-(5,6-dimethoxypyridine-3-carbonyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamide
-
Homo sapiens
[N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-[5-(3-[2-[(3,5-dimethyl-1H-pyrrol-2-yl-kappaN)methylidene]-2H-pyrrol-5-yl-kappaN]propanamido)pentyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamidato](difluorido)boron
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
-
Homo sapiens 5783
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
480000
-
gel filtration Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
palmitoyl-CoA + L-serine Homo sapiens
-
CoA + 3-dehydro-D-sphinganine + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens O15269 AND O15270 AND Q9NUV7 subunit SPT1 and SPT2 and SPT3
-

Source Tissue

Source Tissue Comment Organism Textmining
HCC-4006 cell
-
Homo sapiens
-
non-small cell lung cancer cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
palmitoyl-CoA + L-serine
-
Homo sapiens CoA + 3-dehydro-D-sphinganine + CO2
-
?

Synonyms

Synonyms Comment Organism
serine palmitoyltransferase
-
Homo sapiens
SPT
-
Homo sapiens
SPT1 subunit Homo sapiens
SPT2 subunit Homo sapiens
SPT3 subunit Homo sapiens

Cofactor

Cofactor Comment Organism Structure
pyridoxal 5'-phosphate
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000013
-
subunit SPT2, at pH 8.0 and 25°C Homo sapiens myriocin
0.00000024
-
subunit SPT2, at pH 8.0 and 25°C Homo sapiens [N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-[5-(3-[2-[(3,5-dimethyl-1H-pyrrol-2-yl-kappaN)methylidene]-2H-pyrrol-5-yl-kappaN]propanamido)pentyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamidato](difluorido)boron
0.00000041
-
subunit SPT3, at pH 8.0 and 25°C Homo sapiens myriocin
0.00000076
-
subunit SPT2, at pH 8.0 and 25°C Homo sapiens N-[(7S)-4-(5,6-dimethoxypyridine-3-carbonyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamide
0.0000008
-
subunit SPT2, at pH 8.0 and 25°C Homo sapiens 2-chloro-N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]benzamide
0.0000008
-
subunit SPT3, at pH 8.0 and 25°C Homo sapiens [N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-[5-(3-[2-[(3,5-dimethyl-1H-pyrrol-2-yl-kappaN)methylidene]-2H-pyrrol-5-yl-kappaN]propanamido)pentyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamidato](difluorido)boron
0.0000016
-
subunit SPT3, at pH 8.0 and 25°C Homo sapiens N-[(7S)-4-(5,6-dimethoxypyridine-3-carbonyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]-2-(trifluoromethoxy)benzamide
0.0000041
-
subunit SPT3, at pH 8.0 and 25°C Homo sapiens 2-chloro-N-[(7S)-4-(3,4-dimethoxybenzoyl)-1-(propan-2-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridin-7-yl]benzamide