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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 SMARCA2 degrader-29 is a targeted protein degradation agent designed to selectively degrade the BRM protein. With a DC50 of 10-100 nM for BRM and greater than 1 μM for BRG1 (SMARCA2), this compound offers potent and effective modulation of chromatin remodeling complexes. It is ideal for research applications studying the role of SMARCA2 in cancer biology and epigenetic regulation.
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PROTAC SMARCA2/4-degrader-5 is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and targets SMARCA4 in MV411 with a DC50 ranging from 100 to 500 nM. This compound is instrumental for research applications focused on epigenetic regulation and oncogenic pathways involving SWI/SNF complex alterations.
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PROTAC MLLT1 Degrader-1 is a targeted PROTAC degrader that specifically interacts with MLLT1. This compound effectively inhibits proliferation and viability of acute myeloid leukemia (AML) cells, while also suppressing tumor growth in human AML xenograft models. PROTAC MLLT1 Degrader-1 can be utilized for research focused on MLL-rearranged AML, enabling studies on its oncogene transcriptional regulation and potential therapeutic applications.
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NEP108 is a GID4 E3 ligase-based PROTAC degrader specifically targeting BRD4. With a DC50 value of approximately 3.8 μM, NEP108 demonstrates a strong affinity for GID4, exhibiting a KD value of 0.22 μM, while the KD value for its trimeric complex is 2.85 μM. This compound is suitable for research applications in cancer biology, facilitating the study of BRD4 degradation and its implications in therapeutic strategies.
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PROTAC BRD4 Degrader-22 is a PROTAC-based degrader targeting the bromodomain-containing protein 4 (BRD4). This compound demonstrates significant biological activity with a pDC50 value of 9.2 in MOLT4 cells after 24 hours of treatment. It is primarily utilized in research applications focused on exploring the therapeutic potential of targeted protein degradation in various cancers and other BRD4-related disorders.
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PROTAC SMARCA2/4-degrader-30 is a targeted protein degradation agent specifically designed to degrade the catalytic subunits of the SWI/SNF complex, SMARCA2 and SMARCA4. This compound demonstrates effective degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, with a DC50 of less than 100 nM for both targets. It serves as a valuable tool for investigating the biological roles of SMARCA2 and SMARCA4 in various cancer models and for exploring potential therapeutic strategies in malignant conditions involving these proteins.
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PROTAC BRD4 Degrader-35 is a PROTAC degrader specifically designed to target BRD4. This compound facilitates the ubiquitination and subsequent degradation of BRD4, making it a valuable tool in anti-cancer research. Its mechanism of action enables the modulation of BRD4-dependent pathways, providing insights into the therapeutic potential of BRD4 inhibition in various malignancies.
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PROTAC BRM/BRG1 degrader-3 is a PROTAC-based degrader specifically targeting BRM and BRG1, demonstrating a DC50 value of less than 1 nM for BRM degradation and greater than 1 nM for BRG1 degradation in SW1573 cells. This compound exhibits significant anti-tumor and anti-proliferative activity against A549 cells, with an IC50 of 0.6 nM. Its potent mechanisms make it a valuable tool for investigating the roles of BRM and BRG1 in cancer biology and therapeutic development.
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PROTAC BRM/BRG1 degrader-2 is a potent degrader specifically targeting the BRM/BRG1 proteins via the PROTAC mechanism. It exhibits a DC50 of less than 10 nM in A549 cells, with an IC50 of 15 nM, showcasing its effective biological activity in promoting proteolytic degradation. This compound serves as a valuable tool for researching the roles of BRM/BRG1 in cancer biology and other cellular processes.
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cis-VZ185 is a VHL-based PROTAC that targets and facilitates the degradation of BRD9 and BRD7 proteins. This compound demonstrates efficient and rapid degradation efficiency, making it a valuable tool for studies involving epigenetic regulation and the functional role of bromodomain proteins. cis-VZ185 is suitable for research applications focused on targeted protein degradation and the exploration of novel therapeutic strategies in cancer and other diseases linked to aberrant BRD protein expression.
PROTAC SMARCA2/4-degrader-8 is a specialized PROTAC targeting the catalytic subunit SMARCA2 of the SWI/SNF complex. This compound effectively degrades SMARCA2 with a DC50 of less than 100 nM in A549 cells, while also targeting SMARCA4 with equivalent efficiency in MV411 cells. It serves as a valuable tool in research focused on understanding the roles of these proteins in chromatin remodeling and their implications in various cancer types.
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PROTAC SMARCA2 degrader-5 is a potent degrader specifically designed to target the catalytic subunit SMARCA2 of the SWI/SNF chromatin remodeling complex. This compound effectively induces degradation of SMARCA2 in MV411 and A549 cell lines, demonstrating a DC50 of less than 100 nM, while also degrading SMARCA4 with a DC50 between 100-500 nM. This reagent is essential for researchers investigating the functional role of SMARCA2 and its associated pathways in cancer biology and other cellular processes.
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(S,R)-CFT8634 is a selective PROTAC-class degrader targeting BRD9, designed for oral administration. This compound facilitates the ubiquitination and subsequent degradation of BRD9, which is implicated in various diseases characterized by abnormal cell proliferation. The structure comprises a BRD9 ligand, a CRBN ligase ligand, and a PROTAC linker, enabling effective recruitment of the E3 ligase for degradation. (S,R)-CFT8634 is a valuable tool for investigating BRD9-related biological processes and therapeutic strategies.
PROTAC BRD4 Degrader-34 is a selective degrader that targets the bromodomain-containing protein 4 (BRD4) through a proteolysis-targeting chimera (PROTAC) mechanism. It induces the degradation of the BRD4-BD2 domain via the VHL E3 ubiquitin ligase system. This compound has significant potential for use in cancer research, enabling investigations into the therapeutic effects of targeting BRD4 in oncogenic pathways.
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BRM/BRG1 ATP degrader-1 is a selective degrader targeting BRG1 and BRM, exhibiting IC50 values of 0.01-0.1 μM for BRM degradation and greater than 0.1 μM for BRG1. This compound facilitates the investigation of the functional roles of these proteins in various cellular processes, making it a valuable tool for cancer research. Its mechanism of action provides insights into underlying pathways and mechanisms that may contribute to tumorigenesis.
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PROTAC SMARCA2/4 degrader-37 is a proteolysis-targeting chimera (PROTAC) that selectively degrades SMARCA2 and SMARCA4 proteins. It exhibits a potent inhibitory concentration (IC50) of ≤0.1 μM, highlighting its efficacy in disrupting these bromodomain-containing proteins. This reagent is suitable for applications in cancer research and therapeutic development, particularly in studies involving epigenetic modulation and chromatin remodeling.
PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways.
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment.
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity.
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dTAGV-1 is a selective proteolysis-targeting chimera (PROTAC) degrader designed to target FKBP12F36V-tagged proteins. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studying protein turnover and function. Its application is particularly relevant in cellular and molecular biology research, facilitating the investigation of protein interactions and therapeutic targets.
10-SLF is a PROTAC FKBP12 degrader that facilitates the formation of a ternary complex between FKBP12 and the mutant E3 ligase FBXW7-R465C. This compound promotes the FBXW7-R465C-mediated proteasomal degradation of FKBP12, selectively lowering FKBP12 levels in cells harboring the FBXW7-R465C mutation. 10-SLF is valuable for studying protein degradation pathways and the role of FKBP12 in various biological contexts.
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KB03-SLF is an electrophilic PROTAC degrader targeting DCAF16 to facilitate the degradation of the nuclear protein FKBP12. This compound serves as a valuable tool in cancer research, enabling the investigation of protein homeostasis and degradation pathways. KB03-SLF’s unique structure incorporates specific ligands that enhance its efficacy as a degradative agent, making it a significant asset for studies focused on targeted protein elimination.
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RAFKBP12 is a PROTAC degrader that specifically targets FKBP12, utilizing the CAP-TAC strategy to facilitate proteasome-dependent degradation. This compound operates independently of E3 ubiquitin ligases and protein ubiquitination, demonstrating its innovative mechanism of action. RAFKBP12 serves as a valuable tool for research in protein degradation pathways and therapeutic applications related to FKBP12 modulation.
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PROTAC LRRK2 Degrader-1 is a targeted protein degrader that selectively engages leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 value of less than 10 nM. This compound is designed for the study of LRRK2-mediated pathways and offers significant potential for advancing research on Parkinson's disease. Its ability to induce targeted degradation makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders associated with LRRK2 dysregulation.
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ROTAC LRRK2 degrader-1 is a potent PROTAC degrader targeting LRRK2, a protein associated with neurodegenerative diseases. This compound facilitates the targeted degradation of LRRK2, which is implicated in the pathogenesis of Parkinson’s Disease. ROTAC LRRK2 degrader-1 can be utilized in research to investigate LRRK2-related biological pathways and therapeutic interventions for Parkinson’s Disease and other associated disorders.
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