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
(105)
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von Hippel-Lindau (VHL)
(93)
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MDM2
(8)
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Cereblon
(929)
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IAP
(17)
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KLHDC2
(7)
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Fbxo3
(1)
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RNF4
(2)
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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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KEAP1
(1)
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NEDD4
(1)
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GID4
(1)
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All Product Categories
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Ligands for E3 Ligase Inhibitors
(2)
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Ligands for E3 Ligase Modulators
(2)
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Ligands for E3 Ligase Chemicals
(3)
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Ligands for E3 Ligase Degraders
(2)
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Ligands for E3 Ligase Controls
(4)
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Ligands for E3 Ligase Substrate
(1)
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Ligands for E3 Ligase Ligands
(16)
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Ligands for E3 Ligase Related Products (1205)
Related Products (1205)
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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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Pomalidomide
0 ImagesSynonyms: CC-4047Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
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Lenalidomide
0 ImagesSynonyms: CC-5013Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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CC-885
0 ImagesCC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer.
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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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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.
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MY-1B
0 ImagesMY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
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VH032
0 ImagesVH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs.
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(S,R,S)-AHPC
0 ImagesSynonyms: VH032-NH2; VHL ligand 1(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
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Golcadomide
0 ImagesSynonyms: CC-99282Golcadomide (CC-99282) is a blood-brain barrier-permeable, orally active Cereblon (CRBN) E3 ligase modulator. Golcadomide induces Cereblon to form a closed active conformation, thereby recruiting and triggering the ubiquitin-mediated proteasomal degradation of transcription factors IKZF1, IKZF3, Ikaros and Aiolos. Golcadomide is applicable to research related to relapsed or refractory non-Hodgkin lymphoma, chronic lymphocytic leukemia/small lymphocytic lymphoma, and diffuse large B-cell lymphoma.
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β-Naphthoflavone
0 Imagesβ-Naphthoflavone is an exogenous aryl hydrocarbon receptor (AHR) ligand. β-Naphthoflavone can activate AHR to participate in various biological processes, including cell growth, differentiation, apoptosis, and metabolism. β-Naphthoflavone has antioxidant activity and can exert its antioxidant function by regulating the activity of antioxidant enzymes. β-Naphthoflavone is also a non-carcinogenic CYP1A inducer and can be used to study aristolochic acid (AAI) induced renal injury.
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(S,R,S)-AHPC monohydrochloride
0 ImagesSynonyms: VH032-NH2 monohydrochloride; VHL ligand 1 monohydrochloride(S,R,S)-AHPC (VH032-NH2; VHL ligand 1) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
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(S,R,S)-AHPC-Me
0 ImagesSynonyms: VHL ligand 2; E3 ligase Ligand 1A(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
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Thalidomide 4-fluoride
0 ImagesSynonyms: Cereblon ligand 4; E3 ligase Ligand 4Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
