Literature summary for 5.6.1.3 extracted from

Okumura, H.; Nakazawa, J.; Tsuganezawa, K.; Usui, T.; Osada, H.; Matsumoto, T.; Tanaka, A.; Yokoyama, S.
Phenothiazine and carbazole-related compounds inhibit mitotic kinesin Eg5 and trigger apoptosis in transformed culture cells (2006), Toxicol. Lett., 166, 44-52.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli of C-terminally truncated fragment comprised of amino acids 1-439 fused to glutathione S-transferase	Homo sapiens
the C-terminal truncated fragments of human Eg5 (amino acids 1-439 of human Eg5) fused to GST (E439GST) and amino acids 1-430 of Drosophila conventional kinesin (kinesin heavy chain: KHC) fused to GST (K430GST) are expressed in Escherichia coli	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
1-(3,6-dibromo-9H-carbazol-9-yl)-3-phenethylamino-2-propanol	-	Homo sapiens
1-(3,6-dichloro-9H-carbazol-9-yl)-3-phenethylamino-2-propanol	induces cell death	Homo sapiens
1-phenethylamino-3-phenothiazin-10-yl-propan-2-ol	induces strong mitotic arrest followed by cell death. More than 90% of cells exhibit the monoastral spindle instead of the normal mitotic spindle. Inhibitor selectively kills transformed culture cells; the inhibitor selectively kills transformed cell cultures	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
the C-terminal truncated fragments of human Eg5 (amino acids 1-439 of human Eg5) fused to GST (E439GST) and amino acids 1-430 of Drosophila conventional kinesin (kinesin heavy chain: KHC) fused to GST (K430GST) are expressed in Escherichia coli	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
HeLa cell	-	Homo sapiens	-
HL-60 cell	-	Homo sapiens	-
WI-38 cell	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
kinesin Eg5	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00152	-	pH 6.8, 30°C	Homo sapiens	1-phenethylamino-3-phenothiazin-10-yl-propan-2-ol

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Release 2023.1 (January 2023)