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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.
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies.
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PF15 is a PROTAC designed to target FLT3 kinase through its ligands linked with CRBN. This highly selective FLT3-ITD degrader exhibits a DC50 of 76.7 nM, effectively inhibiting the proliferation of FLT3-ITD-positive cells. PF15 down-regulates the phosphorylation of FLT3 and STAT5, demonstrating significant anti-tumor activity in mouse models, making it a valuable tool for leukemia research.
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dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM). It effectively induces the degradation of these kinases, leading to reduced N-Myc levels and decreased viability in IMR32 neuroblastoma cells. dAurAB5 also downregulates AAK1, PTK2, GAK, and TTK, making it a valuable tool for investigating the molecular mechanisms in neuroblastoma and related cancers.
FAK PROTAC B5 is a potent degrader targeting focal adhesion kinase (FAK) with an IC50 of 14.9 nM. This compound exhibits significant FAK degradation capabilities along with antiproliferative effects. Furthermore, it demonstrates notable plasma stability and moderate membrane permeability, effectively inhibiting cell migration and invasion. FAK PROTAC B5 is suitable for research applications focused on cancer biology and cellular signaling pathways.
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BSJ-04-146 is a selective PROTAC that targets focal adhesion kinase (FAK) for degradation, exhibiting an IC50 of 26 nM. It demonstrates rapid and robust degradation of FAK in cancer cells while maintaining high specificity across the proteome, and it induces prolonged degradation in murine models. The activity of BSJ-04-146 relies on the ubiquitin-proteasome system, making it a valuable tool for investigating pathways associated with pancreatic cancer and triple-negative breast cancer.
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PROTAC TG2 Degrader-3 functions as a targeted protein degrader specifically for transglutaminase 2 (TG2). This compound effectively inhibits the adhesion and migration of ovarian cancer cells, making it a valuable tool for research focused on ovarian cancer biology and therapeutics. By facilitating the degradation of TG2, it provides insights into the modulation of cancer cell behavior and the potential development of novel treatments.
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BI-0319 is a selective PROTAC degrader targeting PTK2/FAK, effectively promoting the degradation of these proteins. This compound has demonstrated the ability to reduce cancer cell viability, inhibit cellular proliferation, and curtail invasion, making it a valuable tool for cancer research, particularly in studies related to liver cancer. BI-0319 provides insights into therapeutic strategies focused on protein degradation in oncology.
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PROTAC c-Met degrader-1 is a selective and orally active degrader targeting c-Met, exhibiting a DC50 of 6.21 nM. This compound promotes CRBN-dependent ubiquitination and subsequent proteasomal degradation of c-Met, effectively inducing G0/G1 phase arrest in c-Met-dependent cancer cells. Furthermore, PROTAC c-Met degrader-1 demonstrates significant anticancer activity by killing c-Met-dependent cells and inhibiting tumor growth in animal models, making it a valuable tool for research in gastric cancer.
OZD-MET 01 is a PROTAC-type MET degrader that utilizes a chaperone-mediated mechanism to induce targeted degradation of the MET protein. It exhibits potent inhibition of cell proliferation in non-small cell lung cancer cell lines H596 and H1437, with IC50 values of 3.07 and 3.5 μM, respectively. This compound serves as a valuable tool for cancer research, particularly in studies investigating MET-targeted therapies and mechanisms of resistance in oncogenic signaling pathways.
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PROTAC c-Met degrader-2 is a PROTAC-based degrader that selectively targets c-Met for degradation through the ubiquitin-proteasome pathway, exhibiting a DC50 of 50 nM. This compound employs a unique linkage incorporating a CRBN ligand derived from Thalidomide, facilitating targeted protein degradation. It serves as a valuable tool for researching c-Met-related pathways and their implications in various cancers, enhancing the understanding of therapeutic strategies involving c-Met modulation.
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PROTAC BTK Degrader-1 is an innovative PROTAC-based compound designed for the selective degradation of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 34.51 nM for wild-type BTK and 64.56 nM for the BTK-481S mutant. This compound effectively lowers BTK protein levels, thereby inhibiting tumor growth. Additionally, PROTAC BTK Degrader-1 features an alkyne group facilitating its application in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for advanced chemical research and targeted therapies.
L18I is a PROTAC designed to target Bruton’s tyrosine kinase (Btk), facilitating the degradation of this protein and thereby mitigating inflammation associated with autoimmune diseases, such as lupus erythematosus induced by BM12 splenocytes. This compound comprises the IBT6A ligand, a linker moiety (Propargyl-PEG3-alcohol), and an E3 ubiquitin ligase ligand (Lenalidomide-Br), effectively promoting the destruction of Btk. L18I serves as a valuable tool for investigating Btk's role in autoimmunity and offers potential pathways for therapeutic intervention.
DD-03-171 is a selective PROTAC BTK degrader that targets Bruton's tyrosine kinase (BTK) for degradation. This compound demonstrates significant anti-proliferative effects on mantle cell lymphoma (MCL) cells with an IC50 of 5.1 nM and enhances survival in murine models bearing patient-derived xenograft (PDX) lymphoma. Additionally, DD-03-171 inhibits platelet function and thrombosis, making it a valuable tool for research in cancer and hematological disorders.
PROTAC BTK Degrader-6 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 of 3.18 nM. This compound exhibits anti-inflammatory activity by inhibiting NF-κB activation and reducing the expression of pro-inflammatory cytokines, including IL-1β and IL-6. It serves as a valuable tool for research into the modulation of immune responses and the development of therapies for inflammatory diseases.
UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM, specifically designed to target Bruton's tyrosine kinase (BTK). It effectively disrupts B-cell receptor signaling and demonstrates robust degradation of both wild-type and mutant BTK proteins, including the C481S mutation. UBX-382 has been shown to inhibit tumor growth in murine xenograft models with BTK-expressing TMD-8 cells, making it a valuable tool for investigating B-cell-related malignancies and therapeutic strategies.
PROTAC BTK Degrader-2 is a highly effective proteolysis-targeting chimera (PROTAC) that selectively degrades Bruton's tyrosine kinase (BTK). By recruiting the Cullin-RING E3 ubiquitin ligase complex, it mediates the ubiquitination and subsequent degradation of BTK protein, leading to a marked reduction in its cellular levels. This compound is valuable in research focused on B-cell malignancies and autoimmune diseases, providing insights into BTK's role in signaling pathways and therapeutic interventions.
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PROTAC BTK Degrader-10 is a PROTAC agent that targets Bruton's Tyrosine Kinase (BTK) for selective degradation. This compound is particularly useful in the study of chronic lymphocytic leukemia (CLL) due to its ability to modulate BTK levels, thereby influencing malignant cell survival and proliferation. The degrader is designed with a specific ligand for BTK and a linker, enabling effective recruitment of the E3 ubiquitin ligase Cereblon for targeted degradation.
SJF620 hydrochloride functions as a PROTAC designed for the degradation of Bruton's tyrosine kinase (Btk) via recruitment of the cereblon (CRBN) E3 ligase. With a DC50 value of 7.9 nM, SJF620 effectively mediates the targeted degradation of Btk, making it a valuable tool for research focused on Btk-related pathways. This compound is particularly relevant in studies of immune responses and various hematological malignancies.
PTD10 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 0.5 nM and a KD of 2.28 nM. It effectively degrades BTK in Ramos and JeKo-1 cell lines, leading to the inhibition of cell growth and the induction of apoptosis through caspase activation and mitochondrial pathways. PTD10 is suitable for investigating mechanisms of B-cell dysregulation and related therapeutic strategies.
DDa-1 is a potent BTK PROTAC degrader with a DC50 of 90 nM, designed to facilitate the targeted degradation of Bruton's Tyrosine Kinase (BTK) in cellular systems. This compound effectively utilizes a novel mechanism involving DCAF1 binding, a distinct linker, and a specific BTK ligand to enhance selectivity and efficacy. DDa-1 is primarily utilized in research applications focusing on BTK-related signaling pathways and therapeutic strategies against B-cell malignancies.
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BCPyr is a PROTAC-class degrader specifically targeting Bruton’s Tyrosine Kinase (BTK), exhibiting a DC50 of 800 nM. This compound integrates a BTK ligand (ligand 11) and an E3 ubiquitin ligase ligand (ligand 20) through a pyrazinyl methanol linker. BCPyr facilitates the targeted degradation of BTK, making it a valuable tool for studying diseases where BTK is implicated, such as certain hematological malignancies.
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PROTAC BTK Degrader-12 is a PROTAC (Proteolysis Targeting Chimera) designed to selectively degrade Bruton's tyrosine kinase (BTK). It facilitates the targeted ubiquitination and subsequent proteasomal degradation of BTK, resulting in diminished signaling pathways associated with B-cell malignancies and autoimmune disorders. This compound serves as a valuable tool in research investigating BTK's role in disease mechanisms and therapeutic interventions.
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TQ-3959 is an orally bioavailable BTK PROTAC degrader that demonstrates a DC50 of 14.6 nM. It exhibits potent antiproliferative effects on both wild-type BTK and the C481S mutant BTK cell lines. In vivo, TQ-3959 effectively inhibits tumor growth in female NOD-SCID mice bearing TMD-8 xenografts. This compound is valuable for investigating B-cell malignancies, including lymphoma.
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PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally bioavailable degrader targeting BTK, IKZF1, and IKZF3 through the PROTAC mechanism. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research, particularly in the context of lymphoma. Its unique mechanism of action allows for the targeted degradation of specific oncogenic proteins, facilitating studies in therapeutic strategies and disease mechanisms.
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PROTAC BTK Degrader-4 is a highly effective PROTAC designed to selectively degrade Bruton's tyrosine kinase (BTK) with a DC50 of less than 100 nM. This compound demonstrates minimal immunomodulatory imide drug (IMiD) activity, with a DC50 of 0.345 μM and a maximum degradation rate of 27.4%. PROTAC BTK Degrader-4 is suitable for investigating various pathologies, including cancers, autoimmune disorders, and inflammatory diseases associated with BTK dysregulation.
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