Ligands for Target Protein for PROTAC
Target Protein-binding Moiety
The PROTAC molecule consists of a target protein ligand and an E3 ubiquitin ligase ligand, with a linker binds them together. The ligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.
Target proteins are usually proteins whose overexpression or accumulation may play important roles in the progress of diseases. Numbers of PROTACs have been developed to degrade kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), epigenetic tools (such as HDAC and BET bromodomain) and E3 ligase themselves (such as MDM2).
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Ligands for Target Protein for PROTAC Inhibitors
(3)
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Ligands for Target Protein for PROTAC Chemicals
(6)
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Ligands for Target Protein for PROTAC Degrader
(1)
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Ligands for Target Protein for PROTAC Controls
(9)
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Ligands for Target Protein for PROTAC Ligands
(14)
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Ligands for Target Protein for PROTAC Related Products (668)
Related Products (668)
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Related Compound Screening Libraries (1)
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Abemaciclib metabolite M18
0 ImagesSynonyms: LSN3106729Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
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Pittsburgh Compound B
0 ImagesSynonyms: PiB; 6-OH-BTA-1Pittsburgh Compound B (PiB) is a blood-brain barrier-permeable, specific Aβ deposition PET tracer that binds to Aβ(1-40) fibrils with a Ki value of 678.4 nM. Through click chemical modification (a clickable Pittsburgh Compound B derivative is prepared by introducing a PEG3 linker and an alkynyl group at the 6-hydroxy site of Pittsburgh Compound B, followed by covalent conjugation with azide-labeled fluorescent dyes or affinity tags via copper-catalyzed azide-alkyne cycloaddition (CuAAC)), Pittsburgh Compound B and its conjugates can be used for fluorescence imaging, ultrastructural studies, and enrichment and characterization of Aβ complexes. Pittsburgh Compound B is applicable to Alzheimer's disease research.
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VUBI1
0 ImagesSynonyms: SOS1 activator 1VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer.
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HJB97
0 ImagesHJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
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iBRD4-BD1
0 ImagesiBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology.
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Ipatasertib-NH2
0 ImagesSynonyms: GDC-0068-NH2; RG7440-NH2
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CS-1-65
0 ImagesSynonyms: Androgen receptor ligand 3CS-1-65 is an androgen receptor (AR) ligand. CS-1-65 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.
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BET-IN-31
0 ImagesBET-IN-31 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
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(S)-SKBG-1
0 Images(S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control..
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Androgen receptor antagonist 1
0 ImagesAndrogen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
