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

Ligands for E3 Ligase

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).

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-A0003
    Lenalidomide 191732-72-6 99.95%
    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-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-101488
    CC-885 1010100-07-8 99.85%
    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-130800
    Eragidomide 1860875-51-9 99.86%
    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-W460193
    N-Me-Thalidomide 4-fluoride 2244520-92-9 99.41%
    N-Me-Thalidomide 4-fluoride is a ligand for E3 ligase, used for the synthesis of Anti-inflammatory agent 70 (HY-157570).
    N-Me-Thalidomide 4-fluoride
  • HY-W440247
    CRBN ligand-109 2758533-77-4 ≥98.0%
    CRBN ligand-109 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-109
  • HY-W244657
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione 191732-74-8
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that can be useful in PROTAC research because it is applicable to the recruitment of the CRBN protein.
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • 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-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-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 99.64%
    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-42424
    (S,R,S)-AHPC-Me hydrochloride 1948273-03-7 99.59%
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) 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 hydrochloride 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.
    (S,R,S)-AHPC-Me hydrochloride
  • 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-101763A
    (S,R,S)-AHPC monohydrochloride 1448189-80-7 99.83%
    (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.
    (S,R,S)-AHPC monohydrochloride
  • HY-146237
    Golcadomide 2379572-34-4
    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
  • HY-W382038
    E3 ligase Ligand 32 2300099-98-1 99.95%
    E3 ligase Ligand 32 (First product in Example 52) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 32 can be connected to the ligand for protein by a linker to form PROTACs and can be used for the synthesis of PROTAC SMARCA2/4-degrader-29 (HY-162743).
    E3 ligase Ligand 32
  • HY-A0003B
    Lenalidomide hemihydrate 847871-99-2 99.98%
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) 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 hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide hemihydrate
  • HY-112078
    (S,R,S)-AHPC-Me 1948273-02-6 99.48%
    (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.
    (S,R,S)-AHPC-Me
  • HY-41547
    Thalidomide 4-fluoride 835616-60-9 99.92%
    Thalidomide 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).
    Thalidomide 4-fluoride
Cat. No. Product Name / Synonyms Application Reactivity

von Hippel-Lindau (VHL)

MDM2

Cereblon

IAP

KLHDC2

Fbxo3

RNF4

DCAF11

DCAF1

UHRF1

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Please try each isoform separately.

Ligands for E3 Ligase Degraders, Ligands, Controls, Inhibitors, Modulators & Chemicals
Product Namevon Hippel-Lindau (VHL)MDM2CereblonIAPKLHDC2Fbxo3RNF4DCAF11DCAF1UHRF1Purity    
Lenalidomide  
Cereblon
       99.95%
Pomalidomide  
Cereblon
       99.96%
CC-885  
Cereblon
Cereblon
       99.85%
Eragidomide  
Cereblon
       99.86%
N-Me-Thalidomide 4-fluoride  
Cereblon
Cereblon
       99.41%
CRBN ligand-109  
Cereblon
       ≥98.0%
Iberdomide  
Cereblon
Cereblon
       99.54%
PT-179  
Cereblon
Cereblon
       99.91%
VH-298
VHL
         99.78%
VH032
VHL
         99.64%
(S,R,S)-AHPC-Me hydrochloride
VHL
         99.59%
(S,R,S)-AHPC
VHL
         99.13%
(S,R,S)-AHPC monohydrochloride
VHL
         99.83%
Golcadomide  
Cereblon
       
E3 ligase Ligand 32
VHL
         99.95%
Lenalidomide hemihydrate  
Cereblon
       99.98%
(S,R,S)-AHPC-Me
VHL
         99.48%
ALV2  
Cereblon
Cereblon
       98.07%
Lenalidomide-Br  
Cereblon
       99.86%
BC-1215     
Fbxo3
    99.93%
ALV1  
Cereblon
       98.62%
VH032-cyclopropane-F
VHL
         99.92%
ZXH-1-161  
Cereblon
Cereblon
       98.43%
(S,S,S)-AHPC hydrochloride
VHL
         99.42%
(S)-Thalidomide  
Cereblon
       99.52%
Lenalidomide-OH  
Cereblon
       99.48%
NV03         
UHRF1
98.82%
VH 101, acid
VHL
         98.37%
Lenalidomide-I  
Cereblon
Cereblon
       99.90%
Biotin-Thalidomide  
Cereblon
       99.65%
(S,R,S)-AHPC-propargyl
VHL
         99.46%
cIAP1 ligand 1   
cIAP1
      99.90%
Nutlin carboxylic acid 
MDM2
        98.63%
VHL-IN-1
VHL
         99.78%
DCAF1 binder 1  
Cereblon
Cereblon
       99.12%
VHL Ligand 8
VHL
         98.04%
CCW16      
RNF4
   98.73%
CC-3060  
Cereblon
Cereblon
       99.7%
VL285
VHL
         98.84%
BMS-986397  
Cereblon
Cereblon
       99.76%
KB02-COOH  
Cereblon
       99.39%
PD 4'-oxyacetic acid  
Cereblon
Cereblon
       99.69%
TD-106  
Cereblon
Cereblon
       99.81%
(S,R,S)-AHPC-Me dihydrochloride
VHL
         99.84%
(S,R,S)-AHPC-Boc
VHL
         
VHL Ligand 14
VHL
         99.93%
AR antagonist 1 hydrochloride
VHL
         99.53%
CRBN modulator-1  
Cereblon
       98.00%
2-Methoxyphenyl dihydrouracil  
Cereblon
       
CC-17369  
Cereblon
       98.68%
(R,S,S)-VH032
VHL
         
Pomalidomide-5-OH  
Cereblon
       99.46%
E3 ligase Ligand 23  
Cereblon
       99.71%
Lenalidomide-F  
Cereblon
       99.89%
OICR-8268  
Cereblon
Cereblon
       
Thalidomide (Standard)  
Cereblon
Cereblon
       
Lenalidomide 5'-piperazine  
Cereblon
Cereblon
       99.92%
CRBN ligand-9  
Cereblon
Cereblon
       ≥98.0%
Thalidomide-piperazine hydrochloride  
Cereblon
       98.27%
Pomalidomide-d3  
Cereblon
Cereblon
       ≥99.0%
VL285 Phenol
VHL
         98.56%
VH 101, thiol
VHL
         98.66%
Lenalidomide (Standard)  
Cereblon
Cereblon
       
E3 ligase Ligand 18  
Cereblon
       99.22%
Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride  
Cereblon
Cereblon
       
Thalidomide-pyrrolidine hydrochloride  
Cereblon
Cereblon
       ≥98.0%
Cereblon inhibitor 1  
Cereblon
       99.19%
Thalidomide-d4  
Cereblon
       98.00%
Lenalidomide-d5  
Cereblon
Cereblon
       99.32%
E3 ligase Ligand 8   
IAP
IAP
      99.32%
Cereblon inhibitor 2  
Cereblon
Cereblon
       98.86%
VH032 thiol
VHL
         
Pomalidomide-6-OH  
Cereblon
       98.09%
Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride  
Cereblon
Cereblon
       98.08%
CRBN ligand-13  
Cereblon
       
(R)-Thalidomide  
Cereblon
       99.80%
Lenalidomide hydrochloride  
Cereblon
       
Pomalidomide-d4  
Cereblon
Cereblon
       
(S,R,S)-AHPC TFA
VHL
         
Aster-A Ligand-3  
Cereblon
       
E3 ligase Ligand 26  
Cereblon
       
E3 ligase Ligand 42  
Cereblon
       
E3 ligase Ligand 22  
Cereblon
       
Pomalidomide-5-O-CH3  
Cereblon
       
E3 ligase Ligand 10   
IAP
IAP
      
DA-PROTAC
VHL
         
(4R,5S)-Nutlin carboxylic acid 
MDM2
        
PROTAC CRBN ligand-2  
Cereblon
       
Thalidomide-(2)piperidine  
Cereblon
Cereblon
       
HOXB7 8–25 
MDM2
        
E3 ligase Ligand 14   
IAP
IAP
      
E3 ligase Ligand 48  
Cereblon
       
E3 ligase Ligand 38  
Cereblon
       
CRBN ligand-17  
Cereblon
       
Lenalidomide-13C5,15N  
Cereblon
Cereblon
       
E3 ligase Ligand 57  
Cereblon
       
(S,R,R)-VH032
VHL
         
E3 ligase Ligand 37
VHL
         
E3 ligase Ligand 36
VHL
         
E3 ligase Ligand PG  
Cereblon, IC50: 2.191 μM
       
(S,R,S)-AHPC-Ala
VHL
         
Pomalidomide-piperazine  
Cereblon
Cereblon
       
Bestatin-amido-Me   
cIAP1
      
E3 ligase Ligand 31  
Cereblon
       
Cyclopropane-(S,R,S)-AHPC
VHL
         
E3 ligase Ligand 44
VHL
         
cis VH-298
VHL
         
E3 ligase Ligand 27
VHL
         
VH032 analogue-2
VHL
         
E3 ligase Ligand 25  
Cereblon
       
(S)-Deoxy-thalidomide-Br  
Cereblon
       
Acepromazine-OTs  
Cereblon
       
E3 ligase Ligand 21  
Cereblon
       
VH032-CH2-Boc
VHL
         
(S)-Deoxy-thalidomide  
Cereblon
Cereblon
       
MV-1-NH-Me   
cIAP1
      
E3 ligase Ligand 13   
IAP
IAP
      
(R)-Pomalidomide-pyrrolidine  
Cereblon
Cereblon
       
(S,R,S,R)-AHPC-Me
VHL
         
CRBN ligand-11  
Cereblon
       
Thalidomide-azetidine-CHO  
Cereblon
Cereblon
       
MY-11B        
DCAF1
 
Ru-Poma  
Cereblon
Cereblon
       
E3 ligase Ligand 45
VHL
         
VH032 analogue-1
VHL
         
BCL-xL/BCL-2 ligand 1
VHL
         
HL389  
Cereblon
       
(3S)Lenalidomide-5-Br  
Cereblon
       
VH032-NH-CO-CH2-NHBoc
VHL
         
GNE7599
VHL
         
tDHU, acid  
Cereblon
Cereblon
       98.83%
Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride  
Cereblon
Cereblon
       
E3 ligase Ligand 34
VHL
         
Me-SJ46411
VHL
         
MEL23 
MDM2
        
OICR-8268-acrylic acid
VHL
         
RR-11055  
Cereblon
Cereblon
       
N-Boc-SBP-0636457-OH   
cIAP1
      
E3 ubiquitin ligase binder-1  
Cereblon
Cereblon
       
Thalidomide-methylpyrrolidine  
Cereblon
Cereblon
       
SJF-0661
VHL
         
(S,R,S)-AHPC-Ac
VHL
         
Pomalidomide-d5  
Cereblon
Cereblon
       
E3 ligase Ligand 33
VHL
         
(S,R,S)-AHPC-O-CF3
VHL
         
(S,R,S)-AHPC dihydrochloride
VHL
         
E3 ligase Ligand 35
VHL
         
SJ46411-Br
VHL
         
E3 ligase Ligand 43
VHL
         
E3 ligase Ligand 7       
DCAF11
  
E3 ligase Ligand 41  
Cereblon
       
AS1411-C4-VH032 
MDM2
        
VHL-SF2
VHL
         
cIAP1 ligand 2   
cIAP1
      
L321  
Cereblon
       
CRBN ligand-1  
Cereblon
Cereblon
       
Pomalidomide-15N,13C5  
Cereblon
Cereblon
       
cIAP1 ligand 4   
IAP
IAP
      
Pomalidomide-6-O-CH3  
Cereblon
       
E3 ligase Ligand 29
VHL
         
SOS1 Ligand intermediate-2
VHL
         
CRBN ligand-181  
Cereblon
       
CRBN ligand-111  
Cereblon
       
CRBN ligand-76  
Cereblon
       
CRBN ligand-148  
Cereblon
       
CRBN ligand-14  
Cereblon
       
AR antagonist 1
VHL
         
CRBN ligand-183  
Cereblon
       
CRBN ligand-110  
Cereblon
       
CRBN ligand-63  
Cereblon
       
3-(5-Bromo-2-chlorophenyl)piperidine-2,6-dione  
Cereblon
       
CRBN ligand-164  
Cereblon
       
CRBN ligand-162  
Cereblon
       
BWA-522 intermediate-1  
Cereblon
Cereblon
       99.27%
3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione  
Cereblon
       
Pomalidomide (Standard)  
Cereblon
Cereblon
       
Phenyl-glutarimide 4'-oxyacetic acid  
Cereblon
Cereblon
       
CRBN ligand-45  
Cereblon
       
SJ6145    
KLHDC2
     
CRBN ligand-112  
Cereblon
       
CRBN ligand-74  
Cereblon
       
CRBN ligand-16  
Cereblon
       
CRBN ligand-84  
Cereblon
       
E3 ligase Ligand 30
VHL
         
Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph
VHL
         
CRBN ligand-47  
Cereblon
       
(S,R,S)-AHPC(Me)-amido-C2-acid
VHL
         
CRBN ligand-83  
Cereblon
       
3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione  
Cereblon
       
SOS1 Ligand intermediate-1
VHL
         
CRBN ligand-108  
Cereblon
       
Thalidomide-5-piperazine  
Cereblon
Cereblon