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 (1352)
Related Products (1352)
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Antibodies (1)
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PROTACs Isoform Comparison
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ZX079
0 ImagesCat. No.: HY-181854CAS No.: 3124583-65-6ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.
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PRO-HD2
0 ImagesCat. No.: HY-155397CAS No.: 3126555-89-0PRO-HD2 is a HDAC6 PROTAC degrader. PRO-HD2 exerts antiproliferative activity in leukemia cells. PRO-HD2 can be used for leukemia research.
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PROTAC CDK2/4/6 Degrader-1
0 ImagesCat. No.: HY-171826CAS No.: 2541626-55-3
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S3D5
0 ImagesCat. No.: HY-179243CAS No.: 3033746-21-0S3D5 is a highly efficient and selective PROTAC degrader targeting STAT3 (KD = 4.35 μM). S3D5 induces degradation of STAT3 in HepG2 cells without significant effects on other STAT proteins. S3D5 exhibits good anti-hepatocellular carcinoma cell proliferation activity, which can be explained by activating the p53 pathway. S3D5 degradation of the STAT3 protein is mediated by the ubiquitin–proteasome system (UPS). S3D5 can be used for the study of hepatocellular carcinoma.
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PROTAC CDK4/6/9 degrader 1
0 ImagesCat. No.: HY-178452CAS No.: 3064994-97-1PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)).
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PROTAC sEH degrader-2
0 ImagesCat. No.: HY-174443PROTAC sEH degrader-2 is a PROTAC targeting degradation agent for soluble epoxide hydrolase (sEH) with pIC50 values of the catalytic domain of 8.37 (human sEH-H) and 7.12 (mouce sEH-H). PROTAC sEH degrader-2 can be used for the research related to inflammation and neuroinflammation, such as Alzheimer's disease.
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PROTAC BTK/IKZF1/3 Degrader-1
0 ImagesCat. No.: HY-179077CAS No.: 2416130-49-7PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))
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PROTAC BRD4 Degrader-51
0 ImagesCat. No.: HY-187372PROTAC BRD4 Degrader-51 is a PROTAC-class degrader targeting BRD4, which degrades BRD4 via the ubiquitin-proteasome pathway. PROTAC BRD4 Degrader-51 degrades BRD4 (long) and BRD4 (short) isoforms with DC50 values of 27.92 nM and 20.03 nM, respectively. PROTAC BRD4 Degrader-51 exhibits antiproliferative activity against tumor cells. It can be used in research related to various cancers such as leukemia and breast cancer.
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Gal-ARV-771
0 ImagesCat. No.: HY-158331CAS No.: 3055593-64-8Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells.
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PROTAC BTK Degrader-4
0 ImagesCat. No.: HY-128408CAS No.: 2893795-12-3PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC50 < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC50 = 0.345 μM, Dmax = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK.
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PROTAC BRM/BRG1 degrader-3
0 ImagesCat. No.: HY-168251CAS No.: 2933125-05-2PROTAC BRM/BRG1 degrader-3 is a BRM/BRG1 PROTAC degrader, exhibiting a DC50 of less than 1 nM for BRM degradation and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 shows moderate inhibitory activity against CYP2D6 and hERG. PROTAC BRM/BRG1 degrader-3 inhibits cancer cell proliferation and tumor tissue growth, and exhibits favorable metabolic stability in liver microsomes. PROTAC BRM/BRG1 degrader-3 can be used in non-small cell lung cancer-related research.
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PROTAC BRM/BRG1 degrader-2
0 ImagesCat. No.: HY-168247CAS No.: 2933124-32-2
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PROTAC GDI2 Degrader-1
0 ImagesCat. No.: HY-156244PROTAC GDI2 Degrader-1 is a GDI2 PROTAC degrader with a DC50 value of 1.48 μM and a Kd value of 23.9 μM. PROTAC GDI2 Degrader-1 triggers paraptosis in tumor cells via endoplasmic reticulum expansion and fusion, endoplasmic reticulum stress, unfolded protein response, and cytoplasmic vacuolization. PROTAC GDI2 Degrader-1 exhibits significant in vivo anti-tumor activity in pancreatic cancer xenograft models. PROTAC GDI2 Degrader-1 can be used for research related to pancreatic cancer.
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SGI-1776-VHL-02
0 ImagesCat. No.: HY-186146CAS No.: 3013618-84-0SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis. SGI-1776-VHL-02 has anti-cancer activity against prostate cancer. SGI-1776-VHL-02 can be used in studies related to prostate cancer.
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SN38-(PEG)2-Pom-α
0 ImagesCat. No.: HY-180555SN38-(PEG)2-Pom-α is a selective PROTAC RPL15 degrader. SN38-(PEG)2-Pom-α induces ubiquitin-mediated degradation of RPL15 without affecting TOP1. SN38-(PEG)2-Pom-α induces damage-associated molecular pattern (DAMP) secretion from cancer cells, which activated cGAS-STING signaling in dendritic cells. SN38-(PEG)2-Pom-α enhances anti-PD-1 immunotherapy in a murine melanoma tumor model expressing human CRBN. SN38-(PEG)2-Pom-α can be used for melanoma research.
