- Signaling Pathways
- PROTAC
- PROTACs
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 (1334)
Related Products (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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TX2-121-1
0 ImagesCat. No.: HY-118998CAS No.: 1603845-42-6TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)). -
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ZS3-046
0 ImagesCat. No.: HY-176457CAS No.: 3087879-97-5 -
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DN1679
0 ImagesCat. No.: HY-181035DN1679 is a potent, selective and orally active CRBN-dependent CDK12/13 PROTAC dual degrader. DN1679 shows DC50 of 8.8/9.8 nM (MDA-MB-231), 5.1/6.4 nM (MDA-MB-157) and 17.2/15.8 nM (MDA-MB-468) for CDK12/13. DN1679 can downregulate DNA damage response gene mRNA levels, such as ATM, ATR, BRCA1 and RAD51. DN1679 demonstrates a potent synergistic anti-tumor effect companied with Olaparib (HY-10162). DN1679 can be used for research of triple-negative breast cance. -
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PROTAC ITK degrader 1
0 ImagesCat. No.: HY-149917PROTAC ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. PROTAC ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. -
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MD-4251
0 ImagesCat. No.: HY-174458MD-4251 is an orally active MDM2 PROTAC degrader with a DC50 of 0.2 nM in RS4;11 cells. MD-4251 induces cereblon-dependent depletion and degradation of MDM2 protein, elevates p53 protein levels and activates p53. MD-4251 inhibits the proliferation of wild-type p53 acute leukemia cells, induces complete and durable tumor regression in xenograft models, and upregulates the protein levels of DSC1, NBEA and CASP14. MD-4251 can be used in studies related to acute leukemia. -
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SMD-6346
0 ImagesCat. No.: HY-184673CAS No.: 3086248-19-0SMD-6346 is an orally active SMARCA2 PROTAC degrader with a DC50 of 3.3 nM. SMD-6346 induces SMARCA2 degradation and exhibits extremely low activity against SMARCA4. SMD-6346 inhibits the growth of SMARCA4-deficient cancer cells and suppresses tumor growth in mouse xenograft models. SMD-6346 can be used for the research of non-small cell lung cancer. -
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LC-1-40
0 ImagesCat. No.: HY-158062LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker). -
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- MS2133
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- PROTAC BRD4 Degrader linker conjugate-2
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PROTAC ERα Y537S degrader-1
0 ImagesCat. No.: HY-145071CAS No.: 2667598-05-0 -
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PROTAC KDM4 degrader-1
0 ImagesCat. No.: HY-173135CAS No.: 3102423-10-6PROTAC KDM4 degrader-1 is a KDM4 PROTAC degrader that degrades KDM4A-C with DC50 values of 37.53, 39.93, and 49.41 nM, respectively, while sparing KDM4D. PROTAC KDM4 degrader-1 induces cell cycle arrest, apoptosis and antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 can be used for the research of esophageal cancer. -
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- PROTAC BRD9 Degrader-5
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DD205-291
0 ImagesCat. No.: HY-168282CAS No.: 3047066-15-6DD205-291 is a selective, orally active HPK1 PROTAC degrader with a DC50 of 8.8 nM. By inducing complete degradation of HPK1 protein, DD205-291 simultaneously blocks both its kinase-dependent functions and non-kinase scaffold functions. DD205-291 inhibits the phosphorylation of SLP-76 with an EC50 of 22.98 nM. DD205-291 induces the production of IL-2 and IFN-γ with EC50 values of 34.68 nM and 32.6 nM, respectively. Combined with anti-PD1 in mouse models, DD205-291 exerts tumor-suppressive effects with favorable safety profiles. DD205-291 can be used in colon cancer-related research. -
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- MS98
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- PROTAC STAT6 degrader-7
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DFCI-002-06
0 ImagesCat. No.: HY-181050CAS No.: 3092208-36-8DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies. -
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- PROTAC STAT6 degrader-8
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KG-FP-003
0 ImagesCat. No.: HY-186117CAS No.: 3066008-42-9KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer. -
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CCT367766
0 ImagesCat. No.: HY-122653CAS No.: 2229856-58-8CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein. -
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CEP1347-VHL-02
0 ImagesCat. No.: HY-168026CEP1347-VHL-02 is a selective MLK3 PROTAC degrader that mediates MLK3 degradation via the ubiquitin-proteasome system, with a DC50 of 50-300 nM. After degrading MLK3, CEP1347-VHL-02 inhibits downstream JNK signaling, induces G2/M phase arrest and apoptosis in cancer cells, and suppresses their clonogenic, migratory and 3D sphere-forming abilities. CEP1347-VHL-02 can be used for the research of triple-negative breast cancer. -
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