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PROTACE3 Ligase Ligand-Linker Conjugate
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. Enabled by the discoveries of high-quality, crystallographically defined ligands for the E3 ligases VHL and CRBN, PROTACs have had a meteoric resurgence in the limelight, a remarkable development that has culminated in the first PROTAC degraders being demonstrated as safe and efficacious in the clinic.
TGN-020
Cited
T510251987-99-6
TGN-020 is an inhibitor of Aquaporin 4 (AQP4, IC50: 3.1 μM), the most abundant water channel in the brain.
- $47
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CitedIberdomide 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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Cited(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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Thalidomide 4'-oxyacetamide-alkyl-C2-amine HCl
T398762341841-02-7
Thalidomide 4'-oxyacetamide-alkyl-C2-amine HCl is an E3 ligase ligand-linker conjugate containing the E3 ubiquitin ligase cereblon (CRBN) and linker for the synthesis of PROTAC.
- $43
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Pomalidomide-C4-OH
T40014
Pomalidomide-C4-OH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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GMB-475
T84882490599-18-1
GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of th
- $88
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Thalidomide-CH2CONH-C3-COOH
T40011
Thalidomide-CH2CONH-C3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Thalidomide-CH2CONH-C2-COOH
T40012
Thalidomide-CH2CONH-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-CH2CONH-C2-COOH
T40006
Pomalidomide-CH2CONH-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-PEG1-CO2H
T400242139348-60-8In house
Pomalidomide-PEG1-CO2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.
- $39
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Thalidomide-O-amido-PEG-C2-NH2 hydrochloride
T188182204226-02-6
Thalidomide-O-amido-PEG-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate, incorporating a Thalidomide-based cereblon ligand and a linker. This compound is used in the synthesis of PROTACs.
- $31
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Pomalidomide-PEG2-NH2 hydrochloride
T40015
Pomalidomide-PEG2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-PEG2-CO2H
T400252140807-17-4
Pomalidomide-PEG2-CO2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.
- $60
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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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Pomalidomide-PEG3-CO2H
T400232138440-82-9
Pomalidomide-PEG3-CO2H (Thalidomide-NH-PEG3-propionic acid) is a synthesized E3 ligase ligand-linker conjugate. Pomalidomide-PEG3-CO2H incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
- $36
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Pomalidomide-C3-NH2 hydrochloride
T400022154342-45-5
Pomalidomide-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that integrates the Pomalidomide-based CRBN ligand and linker used in PROTAC technology.
- $37
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Pomalidomide-C2-COOH
T40005
Pomalidomide-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-C7-NH2 hydrochloride
T400042093387-55-2
Pomalidomide-C7-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $45
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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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Thalidomide-O-amido-C6-NH2 hydrochloride
T188162376990-31-5
Thalidomide-O-amido-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate, integrating a Thalidomide-based cereblon ligand with a linker, suitable for PROTAC synthesis.
- $32
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5-Aminothalidomide
T40017191732-76-0
5-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.
- $34
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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.
- $41
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Boc-NH-PEG3
T7701139115-92-7
Boc-NH-PEG3 (PROTAC Linker 10) is a PEG derivative featuring a hydroxyl group and a Boc-protected amino group, used as a PROTAC linker.
- $35
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Pomalidomide-C6-COOH
T400012225940-50-9
Pomalidomide-C6-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $40
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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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Pomalidomide-C5-COOH
T40007
Pomalidomide-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-C4-COOH
T400092225940-48-5
Pomalidomide-C4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $34
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Pomalidomide-C6-I TFA
T40008
Pomalidomide-C6-I TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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(S,R,S)-AHPC-C3-NH2 hydrochloride
T853342940858-65-9
(S,R,S)-AHPC-C3-NH2 hydrochloride (VH032-C3-NH2 hydrochloride) is an E3 ligase ligand-linker coupler that can be used for the synthesis of PROTAC compounds.
- $34
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Thalidomide-O-CH2CONH-CH2COOH
T40013
Thalidomide-O-CH2CONH-CH2COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Thalidomide-NH-C6-NH2 hydrochloride
T400032375194-37-7
Pomalidomide-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $29
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Pomalidomide-C9-COOH
T400102243000-24-8
Pomalidomide-C9-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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Pomalidomide-C3-I
T40000
Pomalidomide-C3-I is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.
- $68
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(S,R,S)-AHPC-C4-NH2 hydrochloride
T186402245697-83-8
(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate comprising the (S,R,S)-AHPC-based VHL ligand and a linker.
- $32
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Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride
T188192376990-30-4
Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride, incorporating an E3 ligase ligand and a linker, can be used as an immunomodulator for the treatment of cancer.
- $42
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(S,R,S)-AHPC-O-Ph-PEG1-NH-Boc
T186722409007-40-3
(S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is an E3 ligase ligand-linker conjugate designed for targeting the EED protein in PROTAC applications[1].
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Thalidomide-NH-C4-NH2 TFA
T188082093387-50-7
Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate composed of an E3 ligase ligand-linker that integrates a Thalidomide-based cereblon ligand and a linker moiety. This compound is used as a component in PROTAC BRD2 BRD4 degrader-1, a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].
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VHL Ligand-Linker Conjugates 17
T18873
VHL Ligand-Linker Conjugates 17 are chemical compounds that consist of a VHL ligand specialized for the E3 ubiquitin ligase, as well as a PROTAC linker. These conjugates are utilized in the synthesis of various PROTACs, including the notable ARD-266. ARD-266 is an exceptionally effective androgen receptor (AR) PROTAC degrader[1].
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(S,R,S)-AHPC-PEG5-COOH
T188722172820-14-1
(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthetic E3 ligase ligand-linker conjugate developed for PROTAC technology, comprising the (S,R,S)-AHPC-based VHL ligand and a 5-unit PEG linker [1].
- $46
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E3 Ligase Ligand-linker Conjugate 147
T203249
E3 Ligase Ligand-linker Conjugate 147 is a conjugate of an E3 ligase ligand and a PROTAC linker, utilized in the synthesis of BRD9 Degrader-1 (Compound 13-7). Comprising the E3 ligase ligand BRD9 ligand-7 and the PROTAC linker 2-((1R,5S,6s)-3-Azabicyclo[3.1.0]hexan-6-yl)ethan-1-ol, this conjugate plays a critical role in biochemical applications.
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E3 Ligase Ligand-linker Conjugate 122
T2034013033187-29-7
E3 Ligase Ligand-linker Conjugate 122 (Compound 2c) is a conjugate of an E3 ligase ligand and a linker, utilized for the synthesis of the PROTAC degrader NR-11c.
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L321-NH-C3-PEG3-C1-NH2
T203281
L321-NH-C3-PEG3-C1-NH2 is a conjugation of the E3 ligase ligand and linker found in BRD4 PROTAC L134.
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Thalidomide-NH-C2-2-azaspiro[3.3]heptane
T2032832573305-00-5
Thalidomide-NH-C2-2-azaspiro[3.3]heptane is a conjugate of an E3 ubiquitin ligase ligand and a linker, designed for the synthesis of KT-413.
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E3 Ligase Ligand-linker Conjugate 149
T203175
E3 Ligase Ligand-linker Conjugate 149 is an E3 ubiquitin ligase ligand-linker conjugate, and it is used in the synthesis of Setidegrasib.
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E3 Ligase Ligand-linker Conjugate 148
T203611
E3 Ligase Ligand-linker Conjugate 148 is a conjugate used in the synthesis of PROTACs, consisting of an E3 ligase ligand and a linker.
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Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH
T203678
Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH (Compound C6) is a conjugate linking a ligand and an E3 ligase, which is utilized in the synthesis of PROTAC PARP1 degrader-30.
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(S,R,S)-AHPC-C4-NH2 dihydrochloride
T186652341796-78-7
(S,R,S)-AHPC-C4-NH2 dihydrochloride is a chemically derived E3 ligase ligand-linker conjugate that includes the (S,R,S)-AHPC VHL ligand and a linker specifically engineered for EED-Targeted PROTAC[1].
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