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
-
Ligands for E3 Ligase
(106)
View all products
-
von Hippel-Lindau (VHL)
(101)
View all products
-
MDM2
(9)
View all products
-
Cereblon
(937)
View all products
-
IAP
(15)
View all products
-
KLHDC2
(7)
View all products
-
Fbxo3
(1)
View all products
-
RNF4
(3)
View all products
-
DCAF11
(3)
View all products
-
DCAF1
(5)
View all products
-
UHRF1
(1)
View all products
-
TRIM21
(1)
View all products
-
NEURL1B
(1)
View all products
-
KLHL41
(1)
View all products
-
RNF114
(1)
View all products
-
DDB1
(1)
View all products
-
FEM1B
(1)
View all products
-
KEAP1
(1)
View all products
-
NEDD4
(1)
View all products
-
GID4
(1)
View all products
All Product Categories
-
Ligands for E3 Ligase Inhibitors
(2)
View all products
-
Ligands for E3 Ligase Modulator
(1)
View all products
-
Ligands for E3 Ligase Chemicals
(3)
View all products
-
Ligands for E3 Ligase Degraders
(3)
View all products
-
Ligands for E3 Ligase Controls
(4)
View all products
-
Ligands for E3 Ligase Substrate
(1)
View all products
-
Ligands for E3 Ligase Ligands
(16)
View all products
-
Ligands for E3 Ligase Related Products (1227)
Related Products (1227)
-
Antibodies (2)
-
Related Compound Screening Libraries (1)
-
Ligands for E3 Ligase Isoform Comparison
-
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.
-
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.
-
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.
-
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.
-
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.
-
L-Proline
0 ImagesL-Proline is one of the twenty amino acids used in living organisms as the building blocks of proteins.
-
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.
-
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.
-
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.
-
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).
-
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.
-
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.
-
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.
-
(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.
