PROTAC TG2 Degrader-3 is a TG2 PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer. (Pink: Transglutaminase ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).

PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma. (Pink: TEAD1 ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC STAT6 degrader-4 (Compound 3u247) is a STAT6 PROTAC degrader with a DC50 of 0.04 nM. PROTAC STAT6 degrader-4 promotes the ubiquitination and degradation of STAT6, and is applicable to the research of immune diseases.

PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC50 of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.

PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases.

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers. (Pink: Epigenetic Reader Domain Target protein ligand; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker).

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research. (Pink: COX and NF-κB ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).

PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections. (Pink: SARS-CoV Target protein ligand; Blue: VHL ligand ; Black: ).

PROTAC SAMHD1 Degrader-1 is an orally active targeted SAMHD1 PROTAC degrader, with an IC50 of 6.3 μM against the dNTP hydrolase activity of SAMHD1. PROTAC SAMHD1 Degrader-1 binds to SAMHD1 inside cells and mediates its degradation, with low off-target effects. PROTAC SAMHD1 Degrader-1 inhibits the production of pro-inflammatory cytokines and interferes with the cascade amplification process of inflammatory responses. PROTAC SAMHD1 Degrader-1 delays the progression of pulmonary fibrosis and exerts protective effects on lung tissues. PROTAC SAMHD1 Degrader-1 can be used in pulmonary fibrosis-related research. (Pink: Ligands for Target Protein for PROTAC and HIV ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker ).

PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand; Blue: CRBN ligand; Black: Linker).

PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a Kd value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer. (Pink: PLK1 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

NTRK degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). NTRK degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1.NTRK degrader-1 can be used for the research of solid tumors. (Pink: NTRK1 Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).

PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research. (Pink: NAMPT ligand ; Blue: VHL ligand ; Black: linker ).

PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).

PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin (mHTT) PROTAC degrader. PROTAC mHTT Degrader-1 specifically recognizes pathogenic mHTT aggregates and recruits Cereblon (CRBN), thereby inducing ubiquitination and proteasomal degradation of mHTT. PROTAC mHTT Degrader-1 alleviates mHTT-induced cytotoxicity and neuroinflammation. In the R6/2 Huntington's disease mouse model, PROTAC mHTT Degrader-1 reduces cerebral protein aggregation levels and improves body weight, motor coordination and survival rate of animals. PROTAC mHTT Degrader-1 can be used for research on PROTAC therapies for Huntington's disease and other neurodegenerative diseases. (Pink: Huntingtin ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC LRRK2 Degrader-3 (compound 6) is a PROTAC LRRK2 degrader with a DC50 of 0.17 nM. PROTAC LRRK2 Degrader-3 can be used for research in Parkinson’s disease and inflammation. (Pink: LRRK2 ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC LRRK2 Degrader-2 is a PROTAC-based degrader targeting LRRK2 with a DC50 of 0.14 nM. PROTAC LRRK2 Degrader-2 recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, thereby mediating the targeted ubiquitination and subsequent proteasomal degradation of LRRK2. PROTAC LRRK2 Degrader-2 can be used in research related to Parkinson's disease.

PROTAC LRRK2 Degrader-1 (compound 18) is a leucine-rich repeat kinase 2 (LRRK2) PROTAC degrader with an IC50 value less than 10 nM. PROTAC LRRK2 Degrader-1 can be used in the research of Parkinson's disease.

PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance.

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC50 of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis.

PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand; Blue: E3 ligase CRBN ligand; Black: Linker. (Pink: Nur77/NR4A1 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC HyTTD Degrader-1 (Compound B2) is a hydrophobic tag tethered degrader (HyTTD) targeting RET, as well as a degrader of the CCDC6-RET fusion protein. PROTAC HyTTD Degrader-1 induces the degradation of the CCDC6-RET fusion protein via the ubiquitin-proteasome pathway. PROTAC HyTTD Degrader-1 is applicable to the research of RET-driven cancers. (Pink: FLT3 and RET ligand ; Blue: Others ligand ; Black: linker ).

PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2. PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research.

PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer. (Pink: HIF-1α ligand ; Blue: VHL ligand ; Black: linker).

PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia. (Pink: HDAC3 ligand ; Blue: VHL ligand ; Black: linker).

PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII. (Pink: CA Ⅱ ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader (DC50 = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research. (Pink: GPX4 ligand ; Blue: Others ligand ; Black: linker ).

PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer. (Pink: FSP1 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: VHL ligand ; Black: linker).