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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.
Dovitinib-RIBOTAC is an RNA-targeting RIBOTAC degrader that specifically binds to and facilitates the degradation of pre-miR-21. This compound exhibits significant anti-tumor activity and inhibits metastasis in breast cancer models. It serves as a valuable tool for studying the role of miR-21 in cancer biology and therapeutic development.
TDP-43 degrader-1 is a targeted degrader of TDP-43, effective in modulating its cellular distribution. This compound reduces the aggregation of TDP-43-positive HuR stress granules and facilitates the relocalization of aberrantly distributed TDP-43 from the cytoplasm to the nucleus. TDP-43 degrader-1 is a valuable tool in the research of neurodegenerative diseases, including amyotrophic lateral sclerosis and Alzheimer's disease.
PROTAC SMARCA2 degrader-35 is a selective degrader targeting SMARCA2 with a DC50 potency of less than 0.1 μM. This compound exhibits significant anticancer activity by regulating cell proliferation and growth, primarily through mechanisms of cell cycle arrest and inhibition of DNA replication in SMARCA4-deleted cancer cells. It is a valuable tool for research focused on targeted protein degradation and its implications in cancer therapy.
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GSPT1 degrader-2 is a potent molecular glue degrader that targets GSPT1, demonstrating a DC50 of less than 30 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to selectively degrade GSPT1 offers insights into the mechanisms of tumor biology and therapeutic potential in an array of malignancies.
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And1 Degrader 1 is a targeted degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), promoting its degradation in non-small cell lung cancer (NSCLC) cells. At a concentration of 5 μM, And1 Degrader 1, in conjunction with Olaparib at 1 μM, effectively inhibits the proliferation of A549 and H460 cell lines. This compound serves as a valuable tool in cancer research, facilitating the study of And1's role in tumor progression and therapy resistance.
di-Ellipticine-RIBOTAC TFA is a RNase recruiting chimera (RIBOTAC) degrader targeting the expanded G4C2 RNA repeat (r(G4C2)exp). It selectively binds to the three-dimensional structure of r(G4C2)exp, recruiting endogenous ribonuclease to induce cleavage and degradation of this RNA. This compound effectively reduces the levels of the toxic dipeptide repeat proteins derived from the C9orf72 allele, thereby alleviating pathological phenotypes associated with amyotrophic lateral sclerosis and frontotemporal dementia in cellular and murine models. di-Ellipticine-RIBOTAC TFA is valuable for research into ALS and FTD.
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PROTAC GPX4 degrader-5 is a selective degrader targeting GPX4, with a DC50 of 28 nM. This compound effectively induces ferroptosis and enhances reactive oxygen species (ROS) levels while exhibiting low toxicity to normal cells. PROTAC GPX4 degrader-5 demonstrates significant anti-proliferative effects in various tumor cell lines, making it a valuable tool for cancer research.
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PROTAC Chk1 degrader-1 is a selective Chk1-targeting PROTAC that facilitates the recruitment of the Cereblon E3 ligase to promote ubiquitination and subsequent proteasomal degradation of Chk1. This compound effectively induces Chk1 degradation in malignant melanoma cells, demonstrating a robust biological activity without exhibiting a hook effect. PROTAC Chk1 degrader-1 is suitable for research applications focused on understanding the role of Chk1 in malignant melanoma and exploring targeted degradation strategies in cancer therapy.
MMH1 is a novel BRD4 molecular glue degrader that effectively recruits the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). This targeted degradation mechanism allows for the selective reduction of BRD4 levels, which is crucial for studying its role in various biological processes. MMH1 is particularly useful in research applications focusing on cancer biology and epigenetic regulation, enabling the exploration of therapeutic strategies targeting BRD4-associated pathways.
BRD4 degrader-3 is a selective bromodomain-containing protein 4 (BRD4) degrader, showcasing potent activity with IC50 values of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound employs the PROTAC technology to facilitate targeted degradation of BRD4. Additionally, it features an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications in studying BRD4-related pathways and functions.
dBRD 9-A is a selective BRD9 PROTAC degrader that targets the E3 ubiquitin ligase CRBN for the near-complete degradation of BRD9. This compound disrupts BRD9 chromatin binding on a genome-wide scale, leading to downregulation of oncogenic transcriptional programs driven by SS18-SSX and the depletion of GBAF complex members from SS18-SSX complexes. dBRD 9-A also induces cell cycle arrest and promotes apoptosis in synovial sarcoma cells, making it a valuable tool for research focused on synovial sarcoma.
TD-428 is a potent PROTAC designed to target and degrade the BRD4 protein via its connection to Cereblon ligands. With a DC50 value of 0.32 nM, TD-428 exhibits high specificity for BRD4 degradation. This compound combines TD-106, a ligand for CRBN, with JQ1, a BET inhibitor, facilitating effective degradation of BET proteins. TD-428 is valuable for research applications involving cancer biology and epigenetic regulation.
L1BC8 is a BRD4 PROTAC degrader that exhibits significant anticancer activity through targeted degradation of the BRD4 protein. This compound functions as a drug-linker conjugate for antibody-drug conjugates (ADCs), enabling the synthesis of BRD4-degrader antibody conjugates. The resulting conjugates demonstrate potent, antigen-dependent BRD4 degradation and antiproliferative effects in cellular assays, making L1BC8 a valuable tool for cancer research and therapeutic development.
CW-3308 is a potent PROTAC that selectively targets BRD9, facilitating targeted protein degradation. It exhibits significant potential in inhibiting synovial sarcoma, rhabdomyoma, and other BRD9-dependent pathologies. Composed of the BRD9 binding ligand Naphthyridin-Me-dimethoxybenzene-COOH, the linker 3-Azaspiro[5.5]undecane-9-methanol, and the E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine, CW-3308 offers a sophisticated approach for studying protein interactions and degradation pathways in cancer research and beyond.
PROTAC BRD9 Degrader-7 is a selective BRD9-targeting PROTAC that induces BRD9 degradation through the ubiquitin-proteasome pathway, demonstrating a DC50 of 1.02 nM. This compound effectively inhibits cell proliferation in MV4-11 acute myeloid leukemia cells, making it a valuable tool for research in hematologic malignancies and related disorders. Its capacity to modulate BRD9 levels positions it as a promising candidate for studies aimed at understanding the role of this protein in cancer biology.
G-6599 is a monovalent degrader targeting SMARCA2 and SMARCA4, known for its role in regulating chromatin remodeling. This compound covalently binds to a specific cysteine residue in the E3 ligase FBXO22, facilitating the formation of a ternary complex with SMARCA2 and SMARCA4, leading to their efficient degradation through the ubiquitin-proteasome pathway. G-6599 is relevant for research in androgen-dependent prostate cancer and mutant non-small cell lung cancer, providing valuable insights into therapeutic interventions.
YDR1 is a potent SMARCA2 degrader that functions as a PROTAC, exhibiting a DC50 of 7.7 nM. This compound is particularly relevant for research into SMARCA4 mutant cancers, facilitating targeted degradation of SMARCA2. It offers valuable insights into the molecular mechanisms underlying these cancers and aids in the development of novel therapeutic strategies.
CFT-1297 is a BET PROTAC degrader that specifically targets and facilitates the degradation of BRD4. This compound enhances the selective elimination of BRD4 protein, which plays a crucial role in regulating gene transcription associated with various cancers. CFT-1297 serves as a valuable tool for researchers investigating the mechanisms of epigenetic regulation and developing targeted therapies for cancer treatment.
CCW 28-3 is a PROTAC that specifically targets BRD4 for degradation through a proteasome- and RNF4-dependent mechanism. This compound facilitates the targeted removal of BRD4, a critical regulator of gene expression linked to various cancers. Its application in research includes studying the role of BRD4 in transcriptional regulation and therapeutic interventions aimed at modulating oncogenic pathways.
PROTAC BET Degrader-3 is a PROTAC designed to target and degrade BET (bromodomain and extraterminal domain) proteins via the von Hippel-Lindau (VHL) E3 ligase pathway. This compound effectively facilitates the ubiquitination and subsequent proteasomal degradation of BET proteins, altering cellular signaling pathways. It is primarily utilized in research applications focused on cancer biology, epigenetics, and the exploration of therapeutic strategies for BET-related diseases.
PROTAC BRD4 Degrader-9 is a bifunctional degrader targeting the BRD4 protein through a ligase-dependent mechanism using von Hippel-Lindau. It exhibits potent biological activity, effectively degrading BRD4 in PC3 prostate cancer cells with a DC50 of 0.86 nM when conjugated with STEAP1 antibodies and 7.6 nM with CLL1 antibodies. This compound is valuable for research into targeted protein degradation and therapeutic strategies against BRD4-mediated oncogenic processes.
Thalidomide-NH-CBP/p300 ligand 2 is a PROTAC-based degrader that targets the CBP and p300 proteins. This compound facilitates the selective degradation of these transcriptional coactivators, which are implicated in various cancers and other diseases. Its application in research includes the elucidation of the roles of CBP and p300 in transcriptional regulation and therapeutic development for conditions influenced by these proteins.
PROTAC_ERRα is a targeted degrader of the estrogen-related receptor alpha (ERRα), employing a proteolysis-targeting chimera (PROTAC) mechanism for enhanced specificity. This compound induces over 80% proteasomal degradation of ERRα in MCF-7 cells, with a DC50 value of 100 nM. PROTAC_ERRα serves as a valuable tool for investigating the biological functions of ERRα in cancer research and for therapeutic development aimed at ERRα-related pathways.
PROTAC BRD4 Degrader-2 is a proteolysis-targeting chimera (PROTAC) that selectively targets BRD4 and Cereblon. With an IC50 of 14.2 nM against the BRD4 BD1 domain, this compound effectively induces proteasomal degradation of BRD4. It is valuable for research applications investigating the role of BRD4 in transcription regulation, cancer biology, and other diseases associated with aberrant gene expression.
XY-06-007 is a selective and potent bump-and-hole (B&H) PROTAC that degrades BRD4BD1L94V. It exhibits a degradation concentration (DC50) of 10 nM at 6 hours, effectively targeting BRD4BD1L94V without degrading off-target proteins. With favorable pharmacokinetic properties, XY-06-007 is suitable for in vivo studies and serves as a valuable tool for research into BRD4-related pathways and therapeutic applications.
