Ubiquitin Ligase

The attachment of ubiquitin and ubiquitin-like polypeptides to intracellular proteins is a key mechanism in regulating many cellular and organismal processes. Assembly of a chain of at least four ubiquitins linked together via their Lys48 residue marks cellular proteins for degradation by the 26S proteasome. In contrast, monoubiquitination or polyubiquitination with chains linked together via Lys63 serve as nonproteolytic signals in intracellular trafficking, DNA repair, and signal transduction pathways. Ubiquitination of proteins is achieved through an enzymatic cascade involving ubiquitin-activating (E1), ubiquitin-conjugating (E2), and ubiquitin-ligating (E3) enzymes (EC 6.3.2.19). Two major types of E3s exist in eukaryotes, defined by the presence of either a HECT or a RING domain[1]. The SCF (Skp1, Cullins, F-box proteins) multisubunit E3 ubiquitin ligase, also known as CRL (Cullin-RING ubiquitin Ligase) is the largest E3 ubiquitin ligase family that promotes the ubiquitination of various regulatory proteins for targeted degradation, thus regulating many biological processes, including cell cycle progression, signal transduction, and DNA replication[2].


[1] R.J. Deshaies, C.A.P. Joazeiro. RING Domain E3 Ubiquitin Ligases. Annu. Rev. Biochem. 2009, 78, 399-434.
[2]L. Jia et al. SCF E3 ubiquitin ligases as anticancer targets. Curr Cancer Drug Targets. 2011 Mar;11(3):347-56.

14 Item(s)

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Axon ID Name Description From price
2639 AMG 232 Potent, selective, and orally bioavailable MDM2-p53 inhibitor €115.00
1643 HLI 373 HDM2 inhibitor €95.00
1538 JNJ 26854165 HDM2 inhibitor €105.00
1586 JNJ 26854165 dihydrochloride HDM2 inhibitor €105.00
2565 N106 Activator of E1 ligase mediated SERCA2a SUMOylation €95.00
1585 Nutlin-3 MDM2 inhibitor (p53 specific) €95.00
1880 Nutlin-3a Inhibitor of MDM2 €95.00
1881 Nutlin-3b Less potent (+)-enantiomer of Nutlin-3 €90.00
1953 PRT 4165 E3 Ubiquitin ligase Bmi1/Ring1A inhibitor €70.00
2009 RITA Activates p53 through inhibition of MDM2 €105.00
2164 SJ 172550 Small molecule inhibitor of MDMX €95.00
1904 SMER 3 Inhibitor of an SCF family E3 Ubiquitin ligase €90.00
2426 SMURF1 inhibitor A01 Inhibitor of E3 ubiquitin-protein ligase SMURF1 €115.00
2437 SP 141 Specific MDM2 inhibitor with therapeutic effects in breast cancer models €120.00

14 Item(s)

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