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PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.
PROTAC LRRK2 Degrader-2 is designed to target LRRK2 through a PROTAC mechanism, exhibiting a DC50 of 0.14 nM. This compound effectively recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, facilitating targeted ubiquitination and subsequent proteasomal degradation of LRRK2. It serves as a valuable tool for research focused on Parkinson's disease and the study of LRRK2-related pathways.
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker conjugate designed for proteolysis-targeting chimera (PAC) applications, featuring the BRD4 degrader GNE-987 linked via a PEG-based moiety. This compound facilitates targeted protein degradation by utilizing a click chemistry framework, incorporating an azide group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkynylated molecules. Additionally, it supports strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN-functionalized compounds, making it a versatile tool for chemical biology research.
PROTAC hCAII degrader-1 is a highly effective PROTAC targeting human carbonic anhydrase II (hCAII), exhibiting a DC50 of 0.5 nM in HEK293 cells. By recruiting the cereblon (CRBN) E3 ubiquitin ligase, this compound forms a ternary complex that facilitates the ubiquitination and subsequent proteasomal degradation of hCAII. This reagent is critical for research investigating the role of hCAII in various biological processes and therapeutic applications in disease contexts where carbonic anhydrases are implicated.
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader that facilitates the ubiquitination and subsequent proteasomal degradation of SUMO1 proteins. This compound has demonstrated the ability to reduce tumor growth in vivo, making it a valuable tool for cancer research. HB007 is applicable in studies related to brain, breast, colon, and lung cancers, providing insights into the role of SUMOylation in tumorigenesis.
WSB1 Degrader 1 is a potent, orally active degrader of WSB1 (WD repeat and SOCS box-containing 1). It exhibits significant anticancer activity, particularly in the context of metastasis. This compound is useful for research applications aimed at exploring the role of WSB1 in cancer progression and therapeutic strategies targeting WSB1-related pathways.
BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival.
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PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum.
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KG-FP-003 is a potent and selective TEAD PROTAC degrader, demonstrating DC50 values of 6 ± 4 nM for TEAD1, 68 ± 15 nM for TEAD2, 12 ± 5 nM for TEAD3, and 7 ± 5 nM for TEAD4. This compound effectively induces ubiquitination and degradation of TEAD proteins. KG-FP-003 has demonstrated significant anticancer activity against mesothelioma and ovarian cancer, making it a valuable tool for research in cancer biology and therapeutic development targeting TEAD pathways.
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PROTAC TEAD degrader-1 is a targeted molecular degrader that selectively promotes the degradation of transcriptional enhanced associate domain (TEAD) proteins via a ubiquitin-proteasome pathway. With a DC50 value of 54.1 nM in 293T cells, it effectively inhibits cell proliferation in NF2-deficient NCI-H226 cells with an IC50 of 0.21 μM. This compound also modulates the expression of yes-associated protein (YAP) target genes, making it a valuable tool for investigating TEAD-related signaling pathways and their implications in various biological processes.
PROTAC TEAD degrader-2 is a potent degrader designed to target TEAD1 through the proteolysis-targeting chimera (PROTAC) approach. It effectively disrupts the YAP/TAZ-TEAD interaction, exhibiting a low DC50 of 0.6 nM and an IC50 of 1.8 nM. This compound demonstrates strong selective inhibitory activity against YAP-dependent cancer cell lines and significantly reduces transcriptional activity associated with YAP. PROTAC TEAD degrader-2 serves as a valuable tool for investigating the role of TEAD1 in mesothelioma and glioma research.
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PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions.
PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions.
PROTAC eDHFR Degrader-2 selectively targets Escherichia coli dihydrofolate reductase (eDHFR) for degradation. By utilizing a PROTAC mechanism, this compound efficiently promotes the degradation of eDHFR-tagged proteins, making it a valuable tool for studies in protein regulation and degradation pathways. Its ability to modulate protein levels can aid in the investigation of various biological processes and contribute to the development of therapeutic strategies.
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FC-14369 is a PROTAC degrader that selectively targets the HIV-1 Nef protein, exhibiting a DC50 value of 160 nM. By engaging both Nef and the Cereblon E3 ubiquitin ligase, FC-14369 facilitates the ubiquitination and subsequent proteasomal degradation of Nef, leading to the restoration of CD4 and MHC-I expression on the cell surface and effectively inhibiting HIV-1 replication. This compound is valuable for research focused on HIV infection and AIDS, advancing understanding of therapeutic strategies in viral infections.
FC-14367 is a PROTAC degrader that selectively targets the HIV-1 Nef protein. It facilitates the formation of a ternary complex by simultaneously binding to Nef and Cereblon E3 ubiquitin ligase, leading to the ubiquitination and subsequent proteasomal degradation of Nef. This process restores the surface expression of CD4 and MHC-I molecules while effectively inhibiting HIV-1 replication. FC-14367 is valuable for research focused on HIV infection and AIDS pathogenesis.
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PROTAC Hemagglutinin Degrader-1 is a potent degrader specifically targeting influenza hemagglutinin (HA). It exhibits significant biological activity with a median degradation concentration of 1.44 μM, demonstrating broad-spectrum efficacy against influenza viruses. This compound is valuable for research applications focused on viral suppression and the development of antiviral therapeutic strategies.
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HP211206 is a PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2, designed to selectively degrade both the protease and its drug-resistant variants. This compound demonstrates an IC50 of 181.9 nM and a DC50 of 621 nM, reflecting its potency in disrupting viral replication. HP211206 also exhibits antiviral activity, making it a valuable tool for research aimed at understanding and combating SARS-CoV-2 infections.
PROTAC SARS-CoV-2 Mpro degrader-1 is a PROTAC-based degrader specifically targeting the main protease of SARS-CoV-2. This compound exhibits broad-spectrum antiviral activity by promoting the degradation of the protease, which is crucial for viral replication. It serves as a valuable tool in antiviral research and therapeutic development against COVID-19.
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PROTAC SARS-CoV-2 Mpro degrader-2 is a highly effective PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2. This compound exhibits significant antiviral activity against various coronaviruses, including EC50 values of 10.8 μM for SARS-CoV-2, 1.6 μM for HCoV-OC43, and 6.5 μM for HCoV-229E. In Calu-3 cells, it demonstrates potent efficacy with an EC50 of 0.89 μM, making it a valuable tool for research focused on coronavirus biology and potential therapeutic interventions.
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GNE-987 GSH linker-1 is a PROTAC-linker conjugate designed for targeted protein degradation through the chimeric BET degrader GNE-987. Inactive in its original form, GNE-987 GSH linker-1 undergoes disulfide reduction and linker self-immolation to release the active degrader intracellularly. This compound is particularly useful in the study of acute myeloid leukemia, facilitating research into targeted therapeutics for this malignancy.
dASK1 is a selective PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1) through a cereblon (CRBN)-mediated pathway. This compound forms a stable ternary complex with ASK1, promoting its efficient degradation via the ubiquitin-proteasome system. dASK1 exhibits potent activity in degrading ASK1 and serves as a valuable tool in research focused on steatohepatitis and related pathologies.
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KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development.
PROTAC LZK Degrader 1 is a potent PROTAC that selectively induces the degradation of Leucine Zipper Kinase (LZK), encoded by MAP3K13. This compound effectively downregulates the expression of key oncogenes such as p53 and c-MYC, resulting in decreased viability of head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK Degrader 1 is a valuable tool for studying cancer biology and therapeutic strategies targeting LZK. The compound consists of an E3 ligase ligand, a target protein ligand, and a linker, facilitating the targeted degradation mechanism.
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PROTAC DAPK1 Degrader-1 selectively targets DAPK1 for degradation, exhibiting a DC50 value of 119.6 nM. This compound has been shown to elevate MDM2 protein levels while concurrently decreasing cleaved caspase-3 and cleaved PARP levels in a neurotoxin-induced cell apoptosis model. Its ability to effectively inhibit neuronal apoptosis positions PROTAC DAPK1 Degrader-1 as a valuable tool for investigating neurological disorders, including cerebral ischemia and traumatic brain injury.
22-SLF is a PROTAC degrader specifically targeting FK506-binding protein 12 (FKBP12), exhibiting a DC50 of 0.5 µM. This compound forms a ternary complex with C227 and C228 in FBXO22, facilitating FKBP12 degradation in an FBXO22-dependent manner. 22-SLF is a valuable tool for cancer research, serving as a probe to investigate the FBXO22-mediated degradation pathways.
