Ligands for E3 Ligase
E3 ligase-recruiting Moiety
A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.
E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).
Ligands for E3 Ligase Isoform Specific Products
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Ligands for E3 Ligase
(106)
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von Hippel-Lindau (VHL)
(97)
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MDM2
(9)
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Cereblon
(930)
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IAP
(16)
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KLHDC2
(7)
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Fbxo3
(1)
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RNF4
(3)
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DCAF11
(3)
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DCAF1
(5)
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UHRF1
(1)
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TRIM21
(1)
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NEURL1B
(1)
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KLHL41
(1)
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RNF114
(1)
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DDB1
(1)
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FEM1B
(1)
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All Product Categories
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Ligands for E3 Ligase Inhibitors
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Ligands for E3 Ligase Modulators
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Ligands for E3 Ligase Chemicals
(3)
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Ligands for E3 Ligase Degraders
(3)
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Ligands for E3 Ligase Controls
(3)
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Ligands for E3 Ligase Substrate
(1)
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Ligands for E3 Ligase Ligands
(7)
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Ligands for E3 Ligase Related Products (1216)
Related Products (1216)
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Antibodies (2)
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Related Compound Screening Libraries (1)
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Ligands for E3 Ligase Isoform Comparison
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L-Arginine
0 ImagesL-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis.
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Lenalidomide
0 ImagesSynonyms: CC-5013Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
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Glycine
0 ImagesGlycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine inhibits the membrane aggregation of NINJ1 and prevents plasma membrane rupture during cell death. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis.
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E3 ligase Ligand 80
0 ImagesCat. No.: HY-W005799CAS No.: 939-69-5
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N-Methylthalidomide
0 ImagesN-Methylthalidomide is a cereblon ligand derivative that acts as an E3 ubiquitin ligase ligand for the synthesis of PROTAC LLC0424N (HY-185557). LLC0424N serves as a negative control for NSD2 PROTAC degrader LLC0424 (HY-161574), with weak ability to induce NSD2 degradation and low growth inhibitory effect on cancer cells carrying NSD2 mutations.
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L-Proline
0 ImagesL-Proline is one of the twenty amino acids used in living organisms as the building blocks of proteins.
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L-Phenylalanine
0 ImagesL-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
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Iberdomide
0 ImagesSynonyms: CC-220Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
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Eragidomide
0 ImagesSynonyms: CC-90009
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L-Lysine
0 ImagesL-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation.
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Clozapine
0 ImagesClozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
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PT-179
0 ImagesPT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms.
