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).

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 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 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 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).

PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer. (Pink: EZH2 ligand ; Blue: VHL ligand ; Black: linker).

PROTAC EZH2 Degrader-43 (compound 59) is a PROTAC protein degrader targeting EZH2 with an IC50 of 21.73 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-43 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: VHL ligand ; Black: linker).

PROTAC EZH2 Degrader-42 (compound 57) is an EZH2-targeting PROTAC degrader and antiproliferative agent. PROTAC EZH2 Degrader-42 induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-42 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).

PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: cIAP ligand ; Black: ).

PROTAC EZH2 Degrader-40 (compound 56) is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.35 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-40 can be used for the research of diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).

PROTAC EZH2 Degrader-31(compound 69) is a PROTAC protein degrader targeting EZH2, with antiproliferative IC50 values of 3.63 μM in lSU-DHL-6 cells and 8.74 μM in HBL-1 cells. PROTAC EZH2 Degrader-31 can be used for the research of lymphoma. (Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).

PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma. (Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).

PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma. (Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).

PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer. (Pink: EZH2 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research. (Pink: EML4-ALK ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC EGFR degrader 17 (Compound 35) is an EGFR PROTAC degrader with a DC50 value of 0.49 nM. PROTAC EGFR degrader 17 promotes the ubiquitination and degradation of EGFR. PROTAC EGFR degrader 17 can be used in research on various cancers, including non-small cell lung cancer. (Pink: EGFR ligand ; Blue: TNF Receptor ligand ; Black: linker).