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PROTACLigand for E3 Ligase
E3 ligands are an important part of PROTAC (proteolytic targeting chimeric molecule), which together with target protein ligands and linkers constitute PROTAC molecule. It can be a derivative structure of an endogenous ligand peptide segment, or it can be a small molecule compound. Common E3 ligands include CRBN, VHL, IAP and MDM2.
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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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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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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CC-885
Cited
T148931010100-07-8
CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.
- $51
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CitedLenalidomide 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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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 Cited
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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CitedEragidomide
T107651860875-51-9
Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.
- $34
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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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Cited(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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TFC-007
T24870927878-49-7
TFC-007 is a selective and efficient hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, suppressing inflammatory factors. It can be used to synthesize H-PGDS degrader PROTAC (H-PGDS)-1 and study cedar pollen-induced guinea pig allergic rhinitis.
- $64
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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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(S,R,S)-AHPC-Me-C10-NH2 hydrochloride
T18669L2471970-07-5
(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.
- $89
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Avadomide Cited
T35491015474-32-4
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
- $40
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CitedThalidomide 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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Cited(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-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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(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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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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CitedPomalidomide-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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VH032
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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ZXH-1-161
T630102407654-51-5
ZXH-1-161 is a potent Cereblon (CRBN) modulator PROTAC that selectively degrades GSPT1 for use in multiple myeloma research.
- $1,490
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