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 (683)
Related Products (683)
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Related Compound Screening Libraries (1)
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TFC 007
0 ImagesTFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
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Desmethyl-QCA276
0 ImagesSynonyms: PROTAC BRD4-binding moiety 4Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Dasatinib carbaldehyde
0 ImagesSynonyms: BMS-354825 carbaldehyde; PROTAC ABL binding moiety 4Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
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Abemaciclib metabolite M18-d8
0 ImagesCat. No.: HY-126534SPurity: 98.00%Synonyms: LSN3106729-d8Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib 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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SF-1
0 ImagesCat. No.: HY-168545Purity: 99.50%SF-1 is an AURKA ligand that can be used for the synthesis of PROTACs, such as PROTAC MPS1 degrader 2 (HY-168543). SF-1 can act as a free inhibitor and has the ability to pull down AURKA, AURKB, and TTK with DC50 values of 273.5, 933.5, and 1274 nM respectively. SF-1 has an anti-proliferative effect on acute myeloid leukemia.
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PROTAC BRD4 ligand-2 hydrochloride
0 ImagesCat. No.: HY-132942APurity: 99.53%
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(R)-I-BET762 carboxylic acid
0 ImagesSynonyms: (R)-Molibresib carboxylic acid; (R)-GSK525762A carboxylic acid; (R)-PROTAC BRD4-binding moiety 2(R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1.
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MJBIA9836
0 ImagesMJBIA9836 is a MAGE-A3 ligand with a Kd of approximately 8.1 μM. MJBIA9836 elevates MAGE-A3 levels in MAGE-A3-positive cells. MJBIA9836 serves as a Ligand for Target Protein for PROTAC for the synthesis of MAGE-A3 PROTAC degraders, such as KL-465 (HY-169086). MJBIA9836 can be used in the research of MAGE-A3-positive cancers.
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BMS-37
0 ImagesBMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC50 towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC50 between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules.
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Aurora-A ligand 1
0 ImagesAurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma.
