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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 KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers.
TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts.
PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein.
PROTAC BRD9 Degrader-4 is a bifunctional degrader targeting BRD9 through the proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces degradation of BRD9, thereby altering oncogenic pathways associated with various cancers. This compound is utilized in cancer research to study the therapeutic potential of BRD9 modulation and the implications of targeted degradation in tumor biology.
Synonyms: KT-413
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses.
PRO-6E is a PROTAC that targets Cereblon to induce degradation of the MET protein. It achieves up to 81.9% degradation of MET at 1 μM in MKN-45 cells, effectively inhibiting tumor growth both in vitro and in vivo. Additionally, PRO-6E promotes apoptosis and cell cycle arrest, making it a valuable tool for research on MET-related oncogenic processes.
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.
dTAG-13-NEG serves as a negative control for dTAG-13, a PROTAC-based bifunctional degrader that selectively targets FKBP12F36V in the presence of a protein of interest. While dTAG-13 promotes the degradation of FKBP12F36V, dTAG-13-NEG allows for the assessment of specificity and background in experimental setups involving this pathway. This compound is essential for validating experimental results when studying protein degradation mechanisms and their implications in cellular biology.
SMD-3040 is a selective SMARCA2 PROTAC degrader with a DC50 of 12 nM and a maximal degradation efficiency of 91%. This compound effectively inhibits tumor cell proliferation, demonstrating significant antitumor activity. SMD-3040 is particularly useful in studies related to various tumors, including melanoma.
PROTAC BET Degrader-10 is a selective degrader targeting the BET protein BRD4 through a PROTAC mechanism, featuring a DC50 of 49 nM. This compound utilizes ligands for Cereblon and BRD4, promoting the ubiquitination and subsequent degradation of BRD4. It serves as a valuable tool for investigating the role of BRD4 in various biological processes and cancer-related research applications.
NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.
Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology.
KTX-951 is a selective IRAK4 degrader that employs a PROTAC mechanism to facilitate targeted degradation of IRAK4 and IMiD substrates, including Ikaros and Aiolos. With a Kd of 3.5 nM and DC50 values of 13 nM for IRAK4, Ikaros, and Aiolos, KTX-951 demonstrates potent biological activity. It also exhibits an IC50 of 35 nM against OCl-Ly10 CTG, indicating its potential use in antitumor research applications.
PROTAC JAK1 Degrader 1 is a selective PROTAC agent targeting JAK1, exhibiting a DC50 of 214 nM. This compound initiates rapid degradation of JAK1, leading to significant antitumor activity. It serves as a valuable tool for investigating JAK1-related signaling pathways and developing therapeutic strategies for malignancies driven by JAK1 dysregulation.
PROTAC FKBP Degrader-3 is a proteolysis-targeting chimera that utilizes a FKBP ligand binding group and a von Hippel-Lindau (VHL) E3 ligase recruiting moiety linked by a flexible linker. This compound effectively induces the degradation of FKBP12, demonstrating potent biological activity in targeted protein degradation. It is primarily used in research applications related to protein homeostasis, cellular signaling mechanisms, and therapeutic development strategies for modulating protein levels.
MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies.
PROTAC RIPK degrader-6 is a Cereblon-based protein-targeting chimeric molecule designed for the degradation of RIP Kinase. This compound employs a RIP2 kinase inhibitor linked through a suitable spacer to a cereblon ligand, facilitating targeted proteolysis of RIPK. Prominent applications include investigations into kinase-related signaling pathways and the development of innovative therapeutic strategies for diseases associated with RIPK dysregulation.
PROTAC BRD4 Degrader-1 is a novel PROTAC that utilizes ligands for both Cereblon and BRD4, exhibiting an IC50 of 41.8 nM against the BRD4 bromodomain 1 (BD1). This compound promotes the degradation of BRD4 protein, leading to a significant decrease in c-Myc expression. It is designed for research applications aimed at understanding the role of BRD4 in transcriptional regulation and its implications in various cancers.
PROTAC ERRα Degrader-3 is a selective degrader targeting estrogen-related receptor alpha (ERRα) through a von Hippel-Lindau-based mechanism. This compound effectively induces the degradation of ERRα protein by over 80% at a concentration of 30 nM, while showing no activity against ERRβ and ERRγ. It serves as a valuable tool for researchers investigating the role of ERRα in various biological processes and disease states.
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology.
PROTAC EED Degrader-2 is a von Hippel-Lindau-based PROTAC that selectively targets the embryonic ectoderm development (EED) subunit of the polycomb repressive complex 2 (PRC2), exhibiting a pKD of 9.27. This compound acts as an effective inhibitor, demonstrating a pIC50 of 8.11, facilitating the degradation of EED and providing valuable insights for research on PRC2-related epigenetic regulation and its implications in various biological processes. Applications include studies on gene expression regulation and potential therapeutic targets in cancer and developmental biology.
PROTAC IDO1 Degrader-1 is a novel compound targeting indoleamine 2,3-dioxygenase 1 (IDO1) through the engagement of Cereblon E3 ligase, facilitating its ubiquitination and subsequent degradation. With a reported DC50 of 2.84 μM, this degrader enhances the anti-tumor efficacy of HER2 CAR-T cells, making it a valuable tool for research in cancer immunotherapy and targeted degradation methods. Its ability to modulate IDO1 levels opens avenues for investigations into metabolic regulation and tumor microenvironment interactions.
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand.
KB02-JQ1 is a selective PROTAC BRD4 degrader that functions as a molecular glue, specifically targeting BRD4 while sparing BRD2 and BRD3. This compound induces BRD4 degradation by covalently modifying the E3 ligase DCAF16, thereby enhancing the stability and duration of protein degradation in biological systems. Its unique design, which incorporates JQ1 linked to the ubiquitin E3 ligase ligand KB02, facilitates targeted modulation of gene expression, making it a valuable tool for research in cancer biology and therapeutic development.
PROTAC TYK2 degradation agent1 is a selective degrader targeting TYK2, effectively facilitating its degradation with a DC50 value of 14 nM. This compound highlights significant biological activity in modulating TYK2 levels, making it a useful tool for investigating autoimmune diseases. Research applications include studying the role of TYK2 in inflammatory pathways and evaluating potential therapeutic strategies.
