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
All Product Categories
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PROTACs 관련 제품 (1339)
관련 제품 (1339)
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Antibodies (1)
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PROTACs Isoform Comparison
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FAK PROTAC B5
0 ImagesCat. No.: HY-143458CAS No.: 2471525-44-5FAK PROTAC B5 is a FAK PROTAC degrader with an IC50 of 14.9 nM. FAK PROTAC B5 induces FAK degradation via the ubiquitin-proteasome pathway by simultaneously binding to FAK and the CRBN E3 ligase. FAK PROTAC B5 inhibits the proliferation, migration and invasion of cancer cells. FAK PROTAC B5 can be used for the research of non-small cell lung cancer.
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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
0 ImagesCat. No.: HY-173422MS2133 is a VHL-recruiting DOT1L PROTAC degrader. MS2133 possesses antiproliferative activity with a human DOT1L IC50 of 4.6 nM, forms a ternary complex with DOT1L and VHL E3 ligase to drive DOT1L ubiquitination and subsequent proteasomal degradation without affecting DOT1L mRNA transcription, inhibits the proliferation of mixed lineage leukemia-rearranged leukemia cells and downregulates H3K79Me2, restrains proliferation of both tumor and normal cells but lacks cytotoxicity against normal cells, and can be used for the research of mixed lineage leukemia-rearranged leukemia.
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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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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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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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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.
