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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
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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(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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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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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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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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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-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-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-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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(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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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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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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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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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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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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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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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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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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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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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.
- $33
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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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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.
- $51
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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.
- $30
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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.
- $54
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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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(S,R,S)-AHPC-Me-C10-Br
T18668
(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate functioning as a ligand-linker for E3 ligases. This compound incorporates a VHL E3 ligase linker and MS432, derived from the MEK1 2 inhibitor PD0325901[1].
- $81
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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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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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Thalidomide-O-C6-NH2 TFA
T188241957235-99-2
Thalidomide-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[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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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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Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride
T188202245697-84-9
Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, incorporates a cereblon ligand derived from Thalidomide and a 3-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes small molecules to induce protein degradation [1].
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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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Thalidomide-O-amido-C8-NH2 hydrochloride
T18817
Thalidomide-O-amido-C8-NH2 hydrochloride is a synthetic conjugate of an E3 ligase ligand-linker, which combines a cereblon ligand derived from Thalidomide and a linker. It can be utilized in the synthesis of PROTACs[1].
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(S,R,S)-AHPC-C3-NH2
T186642361119-88-0
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized conjugate comprising an E3 ligase ligand-linker and a VH032-based VHL ligand, commonly used in PROTAC technology. This compound is essential in synthesizing various PROTACs, such as UNC6852, a bivalent chemical degrader that specifically targets EED [1].
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Thalidomide-NH-C10-COOH
T18806
Thalidomide-NH-C10-COOH (compound 6b) is a synthetic E3 ligase ligand-linker conjugate, combining the Thalidomide-based von Hippel-Lindau (VHL) ligand with a linker commonly used in PROTAC technology. [1]
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Thalidomide-O-PEG2-propargyl
T188262098487-52-4
Thalidomide-O-PEG2-propargyl (E3 Ligase Ligand-Linker Conjugates 32) is a chemical compound that has been synthesized as a conjugate of an E3 ligase ligand and a linker. It incorporates the cereblon ligand based on Thalidomide, along with a 2-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes ligand-induced protein degradation [1].
- $39
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Thalidomide-PEG2-C2-NH2 hydrochloride
T188112245697-87-2
Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines a Thalidomide-based cereblon ligand with a two-unit PEG linker for use in PROTAC technology[1].
- $84
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Thalidomide-O-amido-C4-NH2 hydrochloride
T188152245697-86-1
Thalidomide-O-amido-C4-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon ligand derived from Thalidomide with a linker and is commonly used in the synthesis of PROTACs[1].
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