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 220.127.116.11). Two major types of E3s exist in eukaryotes, defined by the presence of either a HECT or a RING domain. 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.
 R.J. Deshaies, C.A.P. Joazeiro. RING Domain E3 Ubiquitin Ligases. Annu. Rev. Biochem. 2009, 78, 399-434.
L. Jia et al. SCF E3 ubiquitin ligases as anticancer targets. Curr Cancer Drug Targets. 2011 Mar;11(3):347-56.
|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|