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PROTACLigand for E3 Ligase
A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin–proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands, notably for von Hippel–Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity.
Golcadomide
T637712379572-34-4
Golcadomide (CC-99282) is a orally active CRBN E3 ligase modulator that induces interactions between CRBN and its neo-substrate, recruiting the target disease-causing proteins and the E3 ubiquitin ligase.Golcadomide is used in the study of hematologic malignancies.
- $165
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HaloPROTAC3
T320431799506-07-2
HaloPROTAC3 (HaloPROTAC-3) is a conjugate of ligands for E3 and 16-atom-length linker and a degrader of HaloTag fusion proteins.
- $112
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Lenalidomide
Cited
T1642191732-72-6
Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.
- $36
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Cited(S,R,S)-AHPC hydrochloride
T42071448189-80-7
(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).
- $48
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Pomalidomide Cited
T238419171-19-8
Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.
- $52
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CitedCFT7455
T600242504235-67-8
CFT7455 (Cemsidomide) is an anti-cancer agent showing high affinity to the cereblon E3 ligase with a Kd of 0.9 nM. CFT7455 is an orally active degrader of zinc finger transcription factors Ikaros (IKZF1), and Aiolos (IKZF3).
- $79
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Iberdomide
T77911323403-33-3
Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).
- $39
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Avadomide
T35491015474-32-4
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
- $40
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(S,S,S)-AHPC hydrochloride
T138772115897-23-7
(S,S,S)-AHPC hydrochloride ((S,S,S)-VH032-NH2 hydrochloride) is a VHL amino building block and ligand used as a negative control for (S,R,S)-AHPC. It is based on VH032 and is employed in the recruitment of the VHL protein.
- $38
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(S,R,S)-AHPC
T400282055344-67-5
(S,R,S)-AHPC is a VHL ligand that used in the recruitment of the VHL protein.
- $59
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Eragidomide
T107651860875-51-9
Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.
- $34
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(S,R,S)-AHPC-Me
T77521948273-02-6
(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
- $39
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CC-885
T148931010100-07-8
CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.
- $51
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Thalidomide Cited
T021350-35-1
Thalidomide (Thalomid) is a synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties.
- $50
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CitedVH032
T291061448188-62-2In house
VH032 commonly used as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component.VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs, which can recruit von Hippel-Lindau (VHL) proteins as a ligand of VHL.
- $44
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(S,R,S)-AHPC-PEG3-N3
T179091797406-80-4
(S, R, S)-AHPC-PEG3-N3 (VHL Ligand-Linker Conjugates 8) is a synthesized E3 ligase ligand-linker conjugate. (S, R, S)-AHPC-PEG3-N3 incorporates the (S, R, S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
- $37
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Pomalidomide-PEG4-C2-NH2
T179162225940-52-1
Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and 4-unit PEG linker.
- $30
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Pomalidomide-amino-PEG3-NH2 hydrochloride
T399532380273-75-4
Pomalidomide-amino-PEG3-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a pomalidomide-based cereblon ligand and a linker, which can be used to synthesize PROTACs.
- $40
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BC-1215
T58211507370-20-8
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg mL for IL-1β release).
- $47
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Thalidomide-O-amido-C4-N3
T151892098488-36-7
Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a linker.
- $51
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(S,R,S)-AHPC-PEG1-N3
T179202101200-09-1
(S,R,S)-AHPC-PEG1-N3 (E3 ligase Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that includes the (S,R,S)-AHPC-based VHL ligand and a 1-unit PEG linker used in PROTAC technology.
- $33
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VH-298 Cited
TQ01212097381-85-4
VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.
- $39
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Cited(S,R,S)-AHPC-PEG2-N3
T179132010159-45-0
(S,R,S)-AHPC-PEG2-N3 (VHL Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate comprising a (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker.
- $33
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Thalidomide-O-amido-C6-NH2 TFA
T179191950635-14-9
Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA) is a synthesized E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker.
- $30
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SMER3
T2337167200-34-4
SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.
- $29
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(S,R,S)-AHPC
T84121448297-52-6
(S,R,S)-AHPC (VH032-NH2) is a VH032-based ligand for recruiting the von Hippel-Lindau (VHL) protein, potentially useful for the targeted degradation of the androgen receptor.
- $59
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(S,R,S)-AHPC TFA
T179271631137-51-3
(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.
- $30
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CRBN modulator-1
T88242407829-65-4
CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.
- $33
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Lenalidomide hemihydrate
T22922847871-99-2
Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.
- $29
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Thalidomide 5-fluoride
T9381835616-61-0
Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.
- $29
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Thalidomide 4-fluoride
T7755835616-60-9
Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be 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.
- $29
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Lenalidomide-Br
T180642093387-36-9
Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.
- $29
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Thalidomide-5-OH
T929164567-60-8
Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.
- $29
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Thalidomide-4-OH
T77635054-59-1
Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs
- $29
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5-Aminothalidomide
T40017191732-76-0
5-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.
- $39
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(S,R,S)-AHPC-PEG2-NH2 dihydrochloride
T186752341796-76-5
(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-linker 12) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker[1].
- $34
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Thalidomide-5-methyl
T4050340313-92-6
Thalidomide-5-methyl is a Thalidomide-based cereblon (CRBN) ligand used for the recruitment of CRBN protein.
- $117
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AR antagonist 1
T103591818885-54-9
AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.
- $78
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CRBN ligand-9
T936055003-81-1
CRBN ligand-9 (2-(2,6-dioxopiperidin-3-yl)-5-nitroisoindoline-1,3-dione) exhibit inhibition of CRBN.
- $29
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E3 ligase Ligand 23
T9809444287-56-3In house
E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.
- $31
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Thalidomide-NH-C4-NH-Boc
T188072093388-52-2
Thalidomide-NH-C4-NH-Boc is a synthesized conjugate used in PROTAC technology, combining a Thalidomide-based cereblon ligand with a linker.
- $30
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VH032-cyclopropane-F
T178772306193-99-5
VH032-cyclopropane-F is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.
- $39
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Thalidomide-O-amido-C3-NH2 TFA
T77602022182-58-5
Thalidomide-O-amido-C3-NH2 TFA (Cereblon Ligand-Linker Conjugates 16 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a linker used in PROTAC technology.
- $30
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(S,R,S)-AHPC-Me hydrochloride
T136711948273-03-7
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.
- $34
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Lenalidomide-OH
T180661416990-08-3
Lenalidomide-OH is an analog of Lenalidomide, a cereblon ligand for E3 ubiquitin ligase (CRBN), used for CRBN protein recruitment. It is able to attach to protein ligands using linkers to form PROTAC.
- $42
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VL285
T53341448188-57-5
VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.
- $41
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Pomalidomide-C2-NH2 hydrochloride
T77612305369-00-8
Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and a linker used in [PROTAC] technology.
- $31
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(S,R,S)-AHPC-PEG4-NH2
T15190L2010159-57-4
(S,R,S)-AHPC-PEG4-NH2 (VHL Ligand-Linker Conjugates 4) is a synthetic E3 ligase ligand-linker conjugate, consisting of a VHL ligand based on (S,R,S)-AHPC combined with a 4-unit PEG linker.
- $38
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