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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.
GSPT1 Degrader-6 is a selective degrader targeting GSPT1 through a unique mechanism that promotes the recruitment of the ubiquitin-proteasome system for degradation. With a DC50 value of 13 nM, it demonstrates potent biological activity in modulating GSPT1 levels. This compound is primarily used in research applications focusing on protein homeostasis, cellular stress responses, and the therapeutic modulation of GSPT1-related pathways.
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GSPT2 Degrader-1 is a selective molecular glue designed to target GSPT2 through a unique mechanism of action. This compound combines Thalidomide with the MDEG-541 linker, effectively inducing the degradation of GSPT2 without affecting GSPT1 or MYC. GSPT2 Degrader-1 is valuable for research applications focused on gastrointestinal cancer, offering insights into the role of GSPT2 in tumor biology and potential therapeutic interventions.
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GSPT1 Degrader-5 is a potent GSPT1-targeting molecule that functions as a proteolysis-targeting chimera (PROTAC) with a DC50 of 144 nM. This compound selectively degrades GSPT1, a crucial regulatory protein involved in translation termination and mRNA surveillance. GSPT1 Degrader-5 is valuable for research applications focused on understanding the role of GSPT1 in various cellular processes and its implications in disease models.
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GSPT1 degrader-15 is a selective degrader targeting GSPT1, with a DC50 of 154 nM. This compound demonstrates substantial anti-proliferative effects on leukemia and lymphoma cells, while exhibiting minimal impact on the expression of other proteins. GSPT1 degrader-15 is suitable for research applications focused on leukemia and lymphoma, providing a valuable tool for investigating GSPT1-related pathways in cancer biology.
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P131 is a PROTAC molecule that targets Bruton's tyrosine kinase (BTK) for degradation through the Cereblon ligase complex. This compound is effective in degrading both wild-type and C481S mutant BTK with nanomolar potencies. P131 is utilized in research applications focused on the modulation of BTK activity, providing insights into its role in various B-cell malignancies and related signaling pathways.
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NR-V04 is a selective degrader targeting NR4A1 via a PROTAC mechanism. It facilitates the formation of a ternary complex with NR4A1 and the VHL E3 ligase, promoting proteasome-dependent degradation of NR4A1. Through its action, NR-V04 has been shown to enhance the infiltration of tumor-associated B cells and effector memory CD8+ T cells while decreasing monocytic myeloid-derived suppressor cells within tumor microenvironments. This compound is valuable for research related to melanoma and colon cancer.
ZXH-4-130 TFA is a potent and selective degrader of Cereblon (CRBN), functioning as a CRBN-VHL heterobifunctional protein degrader (PROTAC). This compound exhibits significant biological activity, inducing approximately 80% CRBN degradation at a concentration of 10 nM in MM1.S cells. ZXH-4-130 TFA is a valuable tool for investigating CRBN-mediated pathways and protein degradation mechanisms in various research applications.
MS6105 is a selective LDH-targeted PROTAC that induces the degradation of LDHA and LDHB through the ubiquitin-proteasome system. This compound exhibits notable anticancer activity, making it a valuable tool for cancer research. Additionally, MS6105 features an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, enabling diverse applications in chemical biology and drug discovery.
PROTAC PD-L1 degrader-1 is a CRBN-based protein degrader targeting PD-L1, facilitating the selective degradation of the PD-L1 protein. This compound demonstrates potent PD-L1 degradation in 4T1 cells, with a DC50 value of 0.609 μM. It serves as a valuable tool for investigating therapeutic approaches in breast cancer research.
ERD-3111 is an orally active PROTAC degrader targeting estrogen receptor alpha (ERα) with a reported DC50 of 0.5 nM. This compound effectively inhibits tumor growth in both wild-type MCF-7 xenograft models and in models harboring clinically relevant ESR1 mutations. ERD-3111 is a valuable tool for research focused on estrogen receptor-positive breast cancer, facilitating investigations into targeted degradation pathways and therapeutic strategies.
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROTAC that targets the estrogen receptor (ER). It demonstrates high potency, binding to ER with an IC50 of 0.8 nM, and effectively induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM. This compound is valuable for research applications focused on hormone receptor signaling and targeted protein degradation.
PROTAC VHL-type degrader-1 is a VHL-type PROTAC degrader that facilitates the targeted degradation of the ATM protein. This compound enhances the efficacy of the ATR inhibitor AZD6738 through a synergistic mechanism, making it a valuable tool for investigating the interplay between ATM and ATR signaling pathways. It is applicable in research focusing on cancer therapeutics and cellular response to DNA damage.
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.
