Literature summary for 5.6.1.3 extracted from

Skoufias, D.A.; DeBonis, S.; Saoudi, Y.; Lebeau, L.; Crevel, I.; Cross, R.; Wade, R.H.; Hackney, D.; Kozielski, F.
S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression (2006), J. Biol. Chem., 281, 17559-17569.

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Inhibitors

Inhibitors	Comment	Organism	Structure
S-trityl-L-cysteine	tight binding inhibitor, specific for kinesin Eg5. Inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with a IC50 of 500 nM. The S and D-enantiomers of tritylcysteine are nearly equally potent. No inhibition of KIF2A/Kif2 (kinesin-13 family), KIF2C/MCAK (kinesin-13 family), KIF5B/HsuKHC (kinsin-1 family), KIF19/HsCENP-E (kinesin-7 family), KIF20A/HsRabK6 (kinsin-6 family), KIF22A/HsKid (kinesin-10 family), KIF23/HsMKLP1 (kinesin-6 family), KIFC1/HsKIFC1 (kinesin-14 family)	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + H2O + a kinesin associated with a microtubule at position n	Homo sapiens	-	ADP + phosphate + a kinesin associated with a microtubule at position n+1 (toward the plus end)	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + H2O + a kinesin associated with a microtubule at position n	-	Homo sapiens	ADP + phosphate + a kinesin associated with a microtubule at position n+1 (toward the plus end)	-	?

Synonyms

Synonyms	Comment	Organism
Eg5	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0005	-	tight binding inhibitor, specific for kinesin Eg5. Inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with a IC50 of 500 nM. The S and D-enantiomers of tritylcysteine are nearly equally potent. No inhibition of KIF2A/Kif2 (kinesin-13	Homo sapiens	S-trityl-L-cysteine

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Release 2023.1 (January 2023)