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 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.

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Axon ID Name Description From price
2639 AMG 232 Potent, selective, and orally bioavailable MDM2-p53 inhibitor €120.00
3194 Apcin Inhibitor of APC/C-Cdc20 €110.00
3898 BC-1215 Selective and reversible Fbxo3 inhibitor €99.00
3211 BC1618 Potent, orally bioavailable, and metabolically stable Fbxo48 inhibitor €120.00
3846 C25-140 First-in-class TRAF6–Ubc13 inhibitor €160.00
3763 CFT-7455 Orally active monofunctional degrader for IKZF1/3 Inquire
2935 COH000 First-in-class, highly specific, covalent allosteric inhibitor of SUMO E1 €175.00
3292 dCeMM1 Glue degrader of RBM39 €110.00
3293 dCeMM2 Glue degrader of Cyclin K €100.00
3709 DKM 2-93 Selective inhibitor of UBA5 €70.00
3765 DS-3032 Orally available, potent and selective inhibitor of the p53-MDM2 interaction Inquire
3613 EN219 Covalent RNF114 ligand €120.00
4106 FX12 Selective inhibitor and degrader of RNF5 E3 ubiquitin ligase  Recently added €110.00
1643 HLI 373 HDM2 inhibitor €100.00
3064 HOIPIN 11a Selective, cell-permeable and covalent inhibitor of RBR E3 ubiquitin ligase HOIP €180.00
2972 HOIPIN-8 Potent linear ubiquitin chain assembly complex (LUBAC) inhibitor €130.00
1538 JNJ 26854165 HDM2 inhibitor €105.00
1586 JNJ 26854165 dihydrochloride HDM2 inhibitor €105.00
2939 JTP 0819958 Selective linear ubiquitin chain assembly complex (LUBAC) inhibitor €125.00
2947 JTP 1048196 Prodrug of JTP 0819958; LUBAC inhibitor €125.00
3109 ML-792 Potent and selective inhibitor of SUMO-activating enzyme (SAE) €145.00
2038 MLN4924 Inhibitor of NEDD8 Activating Enzyme (NAE) €60.00
3829 MLN7243 Cell permeable small molecule inhibitor targeting ubiquitin-activating enzymes (UAE, also known as E1 enzymes) Inquire
3466 MT-802 Potent and rapid degrader of BTK; PROTAC €280.00
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
3751 NVP-CGM097 Inhibitor of MDM2 Inquire
3752 NVP-CGM097 dihydrochloride Inhibitor of MDM2 Inquire

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