PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
PROTACs Isoform Specific Products
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PROTACs Related Products (1377)
Related Products (1377)
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Antibodies (1)
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PROTACs Isoform Comparison
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SD-965
0 ImagesCat. No.: HY-182922CAS No.: 3054394-56-5
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PROTAC ERα Degrader-9
0 ImagesCat. No.: HY-163679PROTAC ERα Degrader-9 is a dual-target degrader of estrogen receptor α (ERα) and aromatase (ARO/CYP19A), with a Ki value of 0.25 μM against human ERα and an IC50 value of 4.6 μM against human ARO. PROTAC ERα Degrader-9 degrades ERα and ARO via the ubiquitin-proteasome system, and inhibits the transcriptional activity of ERα and the enzymatic activity of ARO. PROTAC ERα Degrader-9 selectively inhibits cancer cell proliferation, induces cell cycle arrest, and triggers apoptosis. PROTAC ERα Degrader-9 exhibits antiproliferative activity and ERα-degrading activity against cancer cells carrying ERα mutations. PROTAC ERα Degrader-9 can be used in cancer-related research such as breast cancer.
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PROTAC LZK degrader 1
0 ImagesCat. No.: HY-170595CAS No.: 2763268-64-8PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a Kd of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC.
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PROTAC BET Degrader-16
0 ImagesCat. No.: HY-181867CAS No.: 2410947-65-6PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia.
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PROTAC Cdc25 degrader-1
0 ImagesCat. No.: HY-181011PROTAC Cdc25 degrader-1 (Compound D3) is an efficient Cdc25 PROTAC degrader. Its DC50 values for Cdc25A, Cdc25B, and Cdc25C are 0.97, 2.02, and 4.67 μM respectively. PROTAC Cdc25 degrader-1 induces cell cycle arrest and apoptosis in cancer cells and inhibits cell migration ability. PROTAC Cdc25 degrader-1 significantly increases the ROS level. PROTAC Cdc25 degrader-1 can be used for the study of colorectal adenocarcinoma.
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SJYHJ-026
0 ImagesCat. No.: HY-169264SJYHJ-026 is a PROTAC degrader targeting PXR, with a DC50 of 86.6 nM in SNU-C4 HiBiT-PXR KI cells. SJYHJ-026 shows higher selectivity for PXR over CAR, VDR, FXR, LXRα and LXRβ, and can bind to VHL to form a PXR-SJYHJ-026-VHL complex, inducing proteasomal degradation of PXR. SJYHJ-026 blocks agonist-induced PXR-mediated gene expression (including CYP3A4) and reduces basal PXR activity at the CYP3A4 promoter. SJYHJ-026 can be used for the research of colorectal cancer.
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PROTAC IRAK3 degrader-1
0 ImagesCat. No.: HY-142662CAS No.: 2712600-00-3
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PROTAC EZH2 Degrader-44
0 ImagesCat. No.: HY-181413CAS No.: 3093642-25-9PROTAC 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.
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PROTAC tubulin-Degrader-1
0 ImagesCat. No.: HY-162098PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)).
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XF056-132 free base
0 ImagesCat. No.: HY-150400CAS No.: 2407450-73-9Synonyms: MS132NXF056-132 free base (MS132N) is an inactive WDR5 PROTAC degrader with a Kd value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 free base binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 free base can be used in the research of pancreatic ductal adenocarcinoma.
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MTP3
0 ImagesCat. No.: HY-173467MTP3 is a MYC PROTAC Degrator. MTP3 facilitates ternary complex formation with CRBN, driving proteasome-dependent full-length MYC degradation and partially proteasome-independent N-terminal truncated MYC (tMYC) generation. MTP3 induces tMYC formation across multiple cancer cell lines with context-dependent response variability. MTP3 can be used for the research of prostate cancer, breast cancer.
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PROTAC SMARCA2/4 degrader-40
0 ImagesCat. No.: HY-178215CAS No.: 3099581-65-1BRM/BRG1 ligand 4 (Compound 6) is a SMARCA2/4 PROTAC degrader. BRM/BRG1 ligand 4 exhibits potent degradation activity against both SMARCA2 and SMARCA4 in HeLa cells, with DC50 less than 0.1 nM. BRM/BRG1 ligand 4 can be used for the study of cancers associated with SMARCA2/SMARCA4 abnormalities or SWI/SNF mutations.
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YW-N-7 TFA
0 ImagesCat. No.: HY-170855AYW-N-7 TFA is a PROTAC degrader targeting RET kinase, with an IC50 of 8.4 nM. YW-N-7 TFA inhibits RET kinase activity and induces proteasome-mediated degradation of RET fusion proteins, while enhancing the anti-tumor activity of Selpercatinib (LOXO-292) (HY-114370). YW-N-7 TFA can be used in the research of cancers associated with RET gene abnormalities, including medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.
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PROTAC IKKβ degrader-1
0 ImagesCat. No.: HY-181660PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer.
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PROTAC HDAC6 degrader 8
0 ImagesCat. No.: HY-177758PROTAC HDAC6 degrader 8 is a potent and selective HDAC6 PROTAC degrader with a DC50 of 1.94 nM. PROTAC HDAC6 degrader 8 induces HDAC6 degradation in cancer cells with a hook effect, and exerts no impact on other HDAC subtypes, IKZF1, IKZF3 or GSPT1. PROTAC HDAC6 degrader 8 can be used in studies related to multiple myeloma.
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PROTAC USP7 Degrader-2
0 ImagesCat. No.: HY-180793CAS No.: 3056612-67-7PROTAC USP7 Degrader-2 (Compound D16) is an efficient and selective USP7 PROTAC degrader with a DC50 of 1.91 μM (in TE-12 cells). PROTAC USP7 Degrader-2 inhibits the migration of upper gastrointestinal tract (UGI) cancer cells and shows relatively weak anti-proliferative activity. PROTAC USP7 Degrader-2 can be used in the research of metastatic upper gastrointestinal cancer.
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JV8
0 ImagesCat. No.: HY-173433CAS No.: 2841716-61-6JV8 is a BRD4 PROTAC degrader with a target Kd of 0.65 μM. JV8 preferentially induces BRD4 degradation in the cytoplasm via the ubiquitin-proteasome system. JV8 exhibits dose-dependent and time-dependent BRD4 degradation activity and is capable of inducing cell apoptosis. JV8 inhibits tumor growth in a dose-dependent manner and induces BRD4 degradation in tumor tissues in vivo. JV8 can be used in research related to various cancers such as breast cancer and pancreatic cancer.
