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
(12)
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Ligands for Target Protein for PROTAC Related Products (679)
Related Products (679)
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Related Compound Screening Libraries (1)
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PROTAC ERRα ligand 1
0 ImagesPROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERαc, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity.
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Apcin-A
0 ImagesApcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
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ABM-14
0 ImagesABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR.
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PROTAC BET-binding moiety 1
0 ImagesCat. No.: HY-107451CAS No.: 2093387-77-8
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CDK7 ligand 2
0 ImagesCDK7 ligand 2 (Compound A6) is a CDK7 ligand. CDK7 ligand 2 can be used in the synthesis of PROTACs.
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CBP/p300 ligand 3
0 ImagesCat. No.: HY-161483CAS No.: 1936425-34-1CBP/p300 ligand 3 (conpound 3) is a CBP/p300 bromodomain ligand that binds to the CBP and p300 bromodomains with IC50 values of 1.1 nM and 1.3 nM, respectively. CBP/p300 ligand 3 can be used to synthesize CBPD-268 (HY-161369).
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N-piperidine Ibrutinib hydrochloride
0 ImagesN-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
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Desmorpholinyl navitoclax-NH-Me
0 ImagesSynonyms: Desmorpholinyl ABT-263-NH-Me
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HDAC4 ligand-2
0 ImagesCat. No.: HY-W039803CAS No.: 340736-76-7
