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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.
PAK4-IN-6 is a selective degrader of PAK4 (p21-activated kinase 4), functioning through targeted protein degradation mechanisms. This compound serves as a valuable tool in the synthesis of proteolysis-targeting chimeras (PROTACs) and has potential applications in cancer research and therapeutic development. Its ability to modulate PAK4 levels makes it instrumental in studying signaling pathways and cellular processes involving this kinase.
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PROTAC PDIA1 Degrader 1 is a PROTAC-based compound designed to selectively target and degrade PDIA1 through the recruitment of the E3 ligase CRBN. It exhibits significant anticancer activity, effectively inhibiting the proliferation of various cancer cell lines. This compound is a valuable tool for researchers investigating the role of PDIA1 in cancer biology and exploring potential therapeutic strategies for targeting this protein.
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YF135 is a reversible-covalent PROTAC specifically targeting KRAS(G12C). This compound facilitates the degradation of KRAS(G12C) by linking a potent KRAS G12C inhibitor with a VHL ligand scaffold, effectively promoting the proteasomal pathway via E3 ligase VHL. YF135 significantly reduces phospho-ERK levels, making it a valuable tool for research applications focused on KRAS(G12C)-associated pathways in cancer biology.
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SP27 is a PROTAC that selectively degrades Polo-like kinase 4 (PLK4), exhibiting a DC50 of 19.5 nM. This compound is valuable for investigating the role of PLK4 in cellular processes and is particularly relevant in breast cancer research, enabling studies on potential therapeutic applications and mechanisms of action related to oncogenesis.
PROTAC PLK1 Degrader-3 is a PLK1-targeted PROTAC that facilitates the degradation of the Polo-like kinase 1 (PLK1) protein through the N-deglycosylation pathway, exhibiting a dissociation constant (Kd) of 2.2 μM. This compound is primarily utilized in research related to non-small cell lung cancer, enabling investigations into targeted protein degradation mechanisms. While the compound shows limited cell penetration, higher concentrations may be necessary to achieve effective degradation outcomes, making it suitable for various biological studies in oncological contexts.
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PRT3789 is a selective PROTAC degrader targeting SMARCA2, exhibiting a DC50 of 0.72 nM in HeLa cells for SMARCA2 and 14 nM for SMARCA4. By forming a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, PRT3789 facilitates polyubiquitination and subsequent proteasomal degradation of SMARCA2. This compound effectively disrupts the integrity of the SWI/SNF chromatin remodeling complex, leading to the downregulation of oncogenic gene expression, decreased chromatin accessibility, and enhanced expression of genes related to antigen processing and presentation. PRT3789 is applicable in research on SMARCA4-mutated solid tumors, including non-small cell lung cancer, endometrial cancer, and several other malignancies.
NEP202 is a potent SMARCA2 PROTAC degrader that engages the GID4 E3 ligase to facilitate targeted protein degradation. This reagent is valuable for cancer research, enabling the selective degradation of SMARCA2, a key protein implicated in various oncogenic processes. NEP202 offers researchers a powerful tool for studying the role of SMARCA2 in tumor biology and therapeutic responses.
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SMD-1087 is a potent PROTAC that selectively degrades SMARCA2 with a DC50 of 8 nM and SMARCA4 with a DC50 of 1 µM. It combines the E3 ligase ligand (S,R,S)-AHPC-Me, the target protein ligand SMI-1074, and an optimized PROTAC linker, facilitating targeted protein degradation. This compound is valuable for studies investigating the role of SMARCA family proteins in cancer and other diseases by enabling selective modulation of their levels in cellular models.
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PROTAC SMARCA2 degrader-32 is a targeted protein degradation agent that selectively degrades SMARCA2 with a DC50 of 1.3 nM. This compound demonstrates significant inhibitory activity against lung cancer cell line NCI-H838, with a GI50 of 34 nM. Its application in research includes studies on the role of SMARCA2 in cancer biology and therapeutic strategies leveraging PROTAC technology for targeted degradation.
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PROTAC SMARCA2 degrader-24 is a selective degrader targeting the SMARCA2 protein through a PROTAC mechanism. It exhibits potent biological activity with a DC50 value of less than 0.1 µM in HeLa cells, facilitating effective degradation of SMARCA2. Additionally, it demonstrates lower activity against SMARCA4, with a DC50 greater than 10 μM in the same cellular context. This compound serves as a valuable tool for studying the functional roles of SMARCA2 in various biological processes and disease models.
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PROTAC SMARCA2 degrader-22 is a potent proteolysis-targeting chimera (PROTAC) specifically designed to degrade the SMARCA2 protein. It exhibits a degradation efficacy of 94% at a concentration of 100 nM. Additionally, PROTAC SMARCA2 degrader-22 demonstrates effective inhibition of A549 cell proliferation with an EC50 of less than 250 nM, making it a valuable tool for research into cancer biology and therapeutic applications targeting the chromatin remodeling complex.
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PROTAC SMARCA2 Degrader-27 is a proteolysis-targeting chimera (PROTAC) that selectively degrades the SMARCA2 protein. By utilizing a VHL ligand, it engages the ubiquitin-proteasome system to induce targeted degradation of SMARCA2, demonstrating significant potential for research in cancer biology. This compound allows for the investigation of SMARCA2's role in oncogenesis and therapeutic resistance, contributing to the development of novel cancer treatments.
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PROTAC A515 is a targeted protein degradation agent that selectively degradas the SMARCA2 protein. By promoting the ubiquitination of SMARCA2, it facilitates its subsequent degradation via the proteasome pathway. This compound is valuable for cancer research, allowing for the investigation of SMARCA2's role in tumorigenesis and potential therapeutic applications.
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L134 is a potent PROTAC BRD4 degrader that targets BRD4 for ubiquitination and subsequent degradation via the ubiquitin-proteasome pathway, demonstrating a DC50 value of 7.36 nM. This compound operates in a DCAF11-dependent manner, making it a valuable tool for studying BRD4-related signaling and therapeutic applications in cancer and other diseases. As a versatile reagent, L134 supports research in targeted protein degradation and the modulation of gene expression pathways.
MJP6412 is a selective degrader of the histone acetyltransferases p300 and CBP, exhibiting DC50 values of 1.6 nM and 1.2 nM, respectively. This compound effectively induces degradation of these proteins, thereby modulating acetylation levels in cells. MJP6412 is particularly relevant in cancer research, providing insights into the role of p300 and CBP in oncogenic processes and potential therapeutic interventions.
GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It efficiently induces degradation of KDM5B by 68.35% at a concentration of 10 μM through a ubiquitin proteasome-dependent mechanism. This compound elevates H3K4me3 levels and activates type-I interferon signaling pathways in prostate cancer cells, specifically in the 22RV1 cell line. Research applications include studying KDM5B's role in cancer biology and evaluating potential therapeutic strategies that involve epigenetic modulation.
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways.
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PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity.
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PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology.
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PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation.
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PROTAC EZH2 Degrader-17 is a selective protein degrader that targets the enhancer of zeste homolog 2 (EZH2). This compound demonstrates significant antiproliferative activity, with an IC50 of 18.32 μM in lymphoma cell lines. PROTAC EZH2 Degrader-17 is a valuable tool for investigating EZH2-related pathologies and provides insights into the therapeutic potential of protein degradation in cancer research.
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EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies.
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PROTAC EZH2 Degrader-26 is a targeted proteolysis-targeting chimera (PROTAC) designed to specifically degradation of the enhancer of zeste homolog 2 (EZH2). This compound demonstrates a potent inhibitory activity with an IC50 of 5.80 nM against EZH2, alongside micromolar-level activity against EZH1, with an IC50 of 0.06 μM. PROTAC EZH2 Degrader-26 is suitable for research applications involving epigenetic regulation, cancer biology, and studies aimed at understanding histone methylation processes.
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PROTAC EZH2 Degrader-39 is a targeted PROTAC that effectively degrades the EZH2 protein, exhibiting an IC50 of 61.00 nM. This compound functionally inhibits the methyltransferase activity of EZH2, making it an important tool for studying the biological implications of EZH2 modulation. Its applications include cancer research and epigenetic regulation studies, contributing to advancements in targeted therapy development.
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PROTAC EZH2 Degrader-15 is a targeted degrader that specifically interacts with the EZH2 protein via a proteolysis-targeting chimera (PROTAC) mechanism. This compound effectively inhibits the methyltransferase activity of EZH2, leading to its degradation and resulting in alterations to histone methylation patterns. It serves as a valuable tool for research applications focused on epigenetic regulation, cancer biology, and therapeutic strategies aimed at EZH2 modulated pathways.
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