Literature summary for 6.2.1.45 extracted from

Yang, Y.; Kitagaki, J.; Dai, R.M.; Tsai, Y.C.; Lorick, K.L.; Ludwig, R.L.; Pierre, S.A.; Jensen, J.P.; Davydov, I.V.; Oberoi, P.; Li, C.C.; Kenten, J.H.; Beutler, J.A.; Vousden, K.H.; Weissman, A.M.
Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics (2007), Cancer Res., 67, 9472-9481.

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Inhibitors

Inhibitors	Comment	Organism	Structure
4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester	i.e. Pyr-41. Inhibitor blocks loading of immobilized His6-tagged E1 with ubiquitin. PYR-41 does not affect the transfer of ubiquitin to E2 from E1 that is preloaded with ubiquitin, it directly inhibits E1, but not E2 enzymes. In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells. PYR-41 attenuates cytokine-mediated nuclear factor-kappaB activation. This correlates with inhibition of nonproteasomal Lys63 ubiquitylation of TRAF6, which is essential to IkappaB kinase activation	Homo sapiens
4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester	i.e. PYR-41, potential of the inhibitor as therapeutic in cancer	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
2B4-T cell	-	Homo sapiens	-
A-9 cell	-	Homo sapiens	-
HEK-293 Tet-On 3G cell	-	Homo sapiens	-
HeLa cell	-	Homo sapiens	-
JURKAT cell	-	Homo sapiens	-
L-929 cell	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
ubiquitin-activating enzyme E1	-	Mus musculus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
additional information	-	inhibitor blocks loading of immobilized His6-tagged E1 with ubiquitin with an IC50 below 10 microM	Homo sapiens	4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester

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Release 2023.1 (January 2023)