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.
| 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 | Cemsidomide | Orally active monofunctional degrader for IKZF1/3 | €160.00 | |
| 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 | €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 | |
| 4143 | MG degrader compound E14 | Potent molecular glue degrader targeting IKZF1/3, GSPT1 and 2 | €130.00 | |
| 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 | |