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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.
AZ'6421 is a Protcolysis Targeting Chimera (PROTAC) designed to selectively degrade estrogen receptor alpha. It exhibits potent anti-tumor activity, effectively inhibiting uncontrolled cellular proliferation associated with malignancies. AZ'6421 is primarily utilized in cancer research, particularly for investigating breast cancer and its therapeutic strategies.
AD4 is a proteolytic targeting chimera (PROTAC) designed to inhibit PCLAF. This compound effectively degrades PCLAF in RS4;11 cells with an IC50 of 0.6 nM, leading to the activation of the p21/Rb pathway and demonstrating anti-tumor effects. In vivo studies have shown that AD4 prolongs survival in RS4;11-transplanted NOD/SCID mice, highlighting its potential for cancer research applications.
YD54 is a PROTAC designed to induce degradation of the SMARCA2 protein, exhibiting a DC50 of 3.5 nM. This compound utilizes a targeted approach to promote the ubiquitination and proteasomal degradation of SMARCA2, making it a valuable tool for studying SMARCA2-dependent biological processes. YD54 is suitable for applications in cancer research and cellular signaling investigations, where modulation of SWI/SNF complex activity is critical.
JYQ-194 is a proteolysis-targeting chimera (PROTAC) designed to degrade human PARK7, a protein implicated in Parkinson's disease. This reagent serves as a valuable tool for investigating the underlying mechanisms of neurodegeneration and cancer biology. Its ability to selectively target and degrade PARK7 highlights its potential utility in therapeutic applications and biological research related to Parkinson's disease and other neurodegenerative conditions.
PROTAC Axl Degrader 2 is a selective proteolysis-targeting chimera (PROTAC) that degrades Axl with an IC50 of 1.61 μM. This compound exhibits significant anti-proliferation and anti-migration activities in vitro. Additionally, PROTAC Axl Degrader 2 induces mehuosis, making it a valuable tool for studying Axl’s role in cancer progression and therapeutic resistance. Potential research applications include investigations into targeted degradation as a therapeutic strategy in oncology.
PROTAC STAT3 degrader-3 (S3D1) targets the STAT3 protein through a PROTAC-mediated degradation mechanism. This compound exhibits potent anticancer activity by facilitating the ubiquitination and subsequent proteasomal degradation of STAT3, a key oncogenic transcription factor. It is primarily applied in research focused on cancer biology, particularly in studies investigating the therapeutic potential of targeting the STAT3 signaling pathway.
PROTAC TTK degrader-1 is a selective threonine tyrosine kinase (TTK) PROTAC degrader designed to induce target degradation. It demonstrates potent biological activity, with DC50 values of 1.7 nM and 5.8 nM in COLO-205 and HCT-116 cell lines, respectively. This compound exhibits significant anticancer efficacy in xenograft mouse models utilizing COLO-205 human colorectal cancer cells, making it a valuable tool for research in cancer therapeutics and targeted protein degradation.
PROTAC DDR1 degrader-1 is a PROTAC-based degrader designed to selectively target the discoidin domain receptor 1 (DDR1) for proteasomal degradation. This compound utilizes a specific DDR1 inhibitor linked to an E3 ligase ligand, facilitating targeted protein degradation. It exhibits potential applications in elucidating DDR1's role in various cellular processes and disease states, providing valuable insights for therapeutic research.
WH-10417-099 is a CRBN-type PROTAC designed to induce the degradation of over 125 unique kinases through the ubiquitin biotinylation (E-STUB) mechanism. Its structure comprises a PI3Kγ ligand, a Thalidomide 4-fluoride E3 ubiquitin ligase ligand, and an Amino-PEG5-C2-acid linker. This compound is valuable for research into targeted protein degradation and multi-kinase signaling pathways, with potential applications in cancer and other diseases characterized by dysregulated kinase activity.
PROTAC erf3a Degrader-1 is a potent oral degrader designed to target the erf3a protein. This compound exhibits significant anti-proliferative activity against various cancer cell lines, including 22Rv1, making it a valuable tool in cancer research. PROTAC erf3a Degrader-1 is particularly relevant for studies focused on prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia, facilitating the investigation of targeted protein degradation in these malignancies.
CST967 is a USP7 PROTAC degrader that facilitates targeted degradation of the USP7 protein through the ubiquitin-proteasome pathway. By modulating PROTAC concentration, researchers can significantly enhance the degradation rate of USP7, a key regulator in various cellular processes. This compound is valuable in cancer research for investigating the functional consequences of USP7 inhibition and exploring novel therapeutic strategies.
PROTAC SMARCA2 degrader-8 is a selective degrader targeting the SMARCA2 protein, exhibiting a DC50 of 28 nM in A375 cells. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby effectively reducing its cellular levels. It is particularly useful for studies investigating the role of SMARCA2 in various cancer types and for elucidating its mechanisms of action in cellular processes.
ZXH-4-130 is a selective degrader of cereblon (CRBN) utilizing the CRBN-VHL mechanism. This compound effectively facilitates the degradation of target proteins through the ubiquitin-proteasome pathway, making it a valuable tool in studying protein homeostasis and degradation processes. Its applications extend to research in targeted protein degradation and the exploration of CRBN's role in various biological contexts.
MS83 is a novel PROTAC that employs a KEAP1 ligand to target and degrade BRD4, along with its homologs BRD3 and BRD2. By harnessing the ubiquitin-proteasome system, MS83 facilitates targeted protein degradation, providing a powerful tool for dissecting the functional roles of BRD4 in cellular processes. This compound is particularly relevant for research on cancer and epigenetic regulation, offering insights into therapeutic strategies that leverage targeted protein degradation.
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ERK-CLIPTAC is a PROTAC molecule designed to selectively induce the degradation of extracellular signal-regulated kinase (ERK). By harnessing the cellular ubiquitin-proteasome system, it offers a novel approach to modulate ERK activity. This compound is valuable for research applications focused on ERK-related signaling pathways and their implications in various diseases, including cancer and neurodegenerative disorders.
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Photo-lenalidomide-acid is a photochemical agent designed for use in PHOTACs (photo-controllable PROTACs). This compound consists of an E3 ligase ligand linked to a photoswitch and a ligand specific to a protein of interest, allowing precise optical control of protein degradation. Its innovative mechanism facilitates targeted protein modulation in cellular studies and therapeutic applications, making it a valuable tool for researchers investigating protein dynamics.
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CMP98 is a PROTAC designed as a negative control for CM11, targeting the von Hippel-Lindau (VHL) protein. Unlike its active counterparts, CMP98 does not induce degradation of VHL, making it a valuable tool for validating the specificity and efficacy of VHL-dependent degradation studies. This compound can be utilized in research applications involving protein degradation pathways and the exploration of PROTAC mechanisms.
PROTAC ERα Y537S degrader-1 is designed to selectively target and degrade the estrogen receptor-alpha (ERα) variant Y537S by recruiting an E3 ubiquitin ligase. This molecular tool facilitates the modulation of estrogen signaling pathways, providing a research application in the study of hormone-driven cancers. By utilizing a combination of a linker and a protein-binding domain, it enhances the degradation efficiency of the mutant receptor, enabling insights into the role of ERα Y537S in tumor biology and potential therapeutic strategies.
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PROTAC BRD9 Degrader-5 is a proteolysis-targeting chimera (PROTAC) that facilitates the targeted degradation of the bromodomain-containing protein BRD9. This compound employs the cellular ubiquitin-proteasome pathway to promote the selective elimination of BRD9, leading to the modulation of biological pathways associated with cancer and other diseases. It serves as a valuable tool for researchers investigating the role of BRD9 in various cellular processes and therapeutic interventions.
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CCT367766 is a third-generation heterobifunctional PROTAC designed to target and degrade the pirin protein through the CRBN-DDB1 complex. This compound effectively reduces pirin expression at low concentrations, demonstrating an IC50 of 490 nM. It exhibits high binding affinities for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. CCT367766 serves as a valuable chemical tool for probing the biological functions of pirin and advancing research in proteolysis-targeting chimeras.
phoBET1 is a photocaged-PROTAC targeting BRD4 for selective degradation. This compound harnesses light-activated control to induce the degradation of BRD4 protein, resulting in significant suppression of tumor growth. Its unique photocaging mechanism allows for spatial and temporal regulation of protein activity, making it a valuable tool for studying the role of BRD4 in cancer biology and therapeutic applications.
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PROTAC TTK degrader-2 is a potent degrader that targets threonine tyrosine kinase (TTK), demonstrating DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. This compound effectively induces target protein degradation and exhibits anticancer activity in a xenograft mouse model of human colorectal cancer derived from COLO-205 cells. It serves as a valuable tool for investigating TTK's role in cancer biology and may aid in the development of novel therapeutic strategies.
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SIAIS630121-NC is a negative control compound designed for use alongside the NAMPT (nicotinamide phosphoribosyltransferase) PROTAC degrader SIAIS630121. This compound demonstrates no degradation activity on NAMPT, serving as a baseline reference for experimental validation. SIAIS630121-NC is essential for researchers studying the effects of NAMPT degradation and the role of PROTAC technology in targeted protein modulation.
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SMARCA2 degrader-20 is a potent PROTAC that targets the SMARCA2 protein for degradation, exhibiting a DC50 of less than 100 nM in A549 cells. This degrader is valuable for studying the functional consequences of SMARCA2 depletion in cancer biology and epigenetic regulation. Its high efficacy facilitates research into targeted protein degradation strategies and their therapeutic potential in oncology.
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Synonyms: (Rac)-ARV-471
(Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research.
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