2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

Ligands for E3 Ligase

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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 Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-10984
    Pomalidomide 19171-19-8 99.96%
    Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide
  • HY-A0003
    Lenalidomide 191732-72-6 99.94%
    Lenalidomide (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.
    Lenalidomide
  • HY-101488
    CC-885 1010100-07-8 99.26%
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.
    CC-885
  • HY-14658
    Thalidomide 50-35-1 99.98%
    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide
  • HY-N0486
    L-Leucine 61-90-5 99.79%
    L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
    L-Leucine
  • HY-W593794
    E3 ligase Ligand 79 2152672-96-1 99.07%
    E3 ligase Ligand 79 is a CRBN E3 ligase ligand that can be used for synthesis of PROTACs.
    E3 ligase Ligand 79
  • HY-185142
    (S,R,S)-AHPC-Me-C8-NHS ester 99.89%
    The (S,R,S)-AHPC-Me-C8-NHS ester is an E3 ubiquitin ligase VHL ligand, used to recruit the VHL protein. The (S,R,S)-AHPC-Me-C8-NHS ester can be linked to the target protein ligand through a linker to form a PROTAC.
    (S,R,S)-AHPC-Me-C8-NHS ester
  • HY-185391
    DCAF1 ligand 2
    DCAF1 ligand 2 (Tert-butyl (2-((2-(1-(4-chlorophenyl)cyclohexyl)-7-(piperazin-1-yl)quinazolin-4-yl)amino)ethyl)carbamate) is a ligand of the E3 connecting enzyme DCAF1. DCAF1 ligand 2 can be used for the synthesis of PROTACs.
    DCAF1 ligand 2
  • HY-N0215
    L-Phenylalanine 63-91-2 99.98%
    L-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.
    L-Phenylalanine
  • HY-101291
    Iberdomide 1323403-33-3 99.54%
    Iberdomide (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.
    Iberdomide
  • HY-130800
    Eragidomide 1860875-51-9 99.93%
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation.
    Eragidomide
  • HY-N0004
    Oridonin 28957-04-2 99.89%
    Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
    Oridonin
  • HY-14539
    Clozapine 5786-21-0 99.84%
    Clozapine (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).
    Clozapine
  • HY-160695
    PT-179 2924858-25-1 99.91%
    PT-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.
    PT-179
  • HY-N0832
    L-Histidine 71-00-1 99.97%
    L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.
    L-Histidine
  • HY-100947
    VH-298 2097381-85-4 99.78%
    VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs.
    VH-298
  • HY-120217
    VH032 1448188-62-2 99.43%
    VH032 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.
    VH032
  • HY-125845
    (S,R,S)-AHPC 1448297-52-6 99.13%
    (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.
    (S,R,S)-AHPC
  • HY-122542B
    PPACK TFA 157379-44-7 99.80%
    PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
    PPACK TFA
  • HY-146237
    Golcadomide 2379572-34-4 98.04%
    Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).
    Golcadomide
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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