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 (1398)
Related Products (1398)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC HDAC6/ERα degrader 1
0 ImagesCat. No.: HY-187387CAS No.: 3092711-76-4PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC50 values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research.
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Dth
0 ImagesCat. No.: HY-175397Synonyms: DFHBI-thalidomideDth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research.
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PROTAC c-Met degrader-5
0 ImagesCat. No.: HY-175320PROTAC c-Met degrader-5 is an orally active c-Met PROTAC degrader. PROTAC c-Met degrader-5 induces c-Met degradation via Cullin-CRBN, with a DC50 value of 0.32 nM, and inhibits the phosphorylation of c-Met and its downstream signaling molecule STAT3. PROTAC c-Met degrader-5 inhibits cancer cell proliferation, migration and invasion, induces apoptosis, alters cell cycle distribution, and suppresses the growth of EBC-1 xenograft tumors. PROTAC c-Met degrader-5 can be used to study MET-driven cancers as well as Tepotinib (HY-14721)-resistant cancers harboring c-MetD1228N and c-MetY1230H mutations.
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PROTAC 20S proteasome subunit β5 degrader 2
0 ImagesCat. No.: HY-169135PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasome. PROTAC 20S proteasome subunit β5 degrader 2 exerts antiproliferative effects in cancer cells and exhibits antitumor activity both in vitro and in vivo. It can be used for the research of pharyngeal cancer and drug-resistant multiple myeloma.
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PROTAC 11β-HSD1 Degrader 1
0 ImagesCat. No.: HY-179602PROTAC 11β-HSD1 Degrader 1 is a highly efficient PROTAC targeting 11β-HSD1 (Hydroxysteroid 11-beta dehydrogenase 1). PROTAC 11β-HSD1 Degrader 1 demonstrates ubiquitin-proteasome-dependent degradation of 11β-HSD1. PROTAC 11β-HSD1 Degrader 1 can be used for the study of type 2 diabetes mellitus (T2DM).
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PROTAC sEH degrader-5
0 ImagesCat. No.: HY-187425CAS No.: 3123230-60-1PROTAC sEH degrader-5 is a highly efficient PROTAC degrader that targets and degrades soluble epoxide hydrolase (sEH) by recruiting cereblon. PROTAC sEH degrader-5 directly inhibits the hydrolase activity of human and mouse sEH, with pIC50 values of 10.36 and 8.41, respectively. PROTAC sEH degrader-5 alleviates LPS (HY-D1056)-induced acute inflammation in vivo. PROTAC sEH degrader-5 can be used in studies related to LPS-induced acute inflammation.
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LC-MI-3
0 ImagesCat. No.: HY-162538CAS No.: 3053823-69-8LC-MI-3 is an orally active IRAK4 PROTAC degrader with an IC50 of 57.2 nM and high selectivity among human protein kinases. LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems. LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways. LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases.
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PROTAC TEAD degrader-2
0 ImagesCat. No.: HY-186021CAS No.: 2918762-17-9PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma.
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PROTAC RIPK2 Degrader-1
0 ImagesCat. No.: HY-147235CAS No.: 2143956-20-9RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases.
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GNE-1567
0 ImagesCat. No.: HY-175448GNE-1567 is a potent ERα PROTAC degrader and a XIAP antagonist with a Kd of 0.03 μM. GNE-1567 induces ubiquitination and degradation of ERα by recruiting the E3 ubiquitin ligase XIAP, thereby achieving the dual effects of ERα protein elimination and abrogation of XIAP-mediated apoptosis inhibition simultaneously. GNE-1567 can be used in studies related to ERα-dependent breast cancer.
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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 soluble epoxide hydrolase (sEH) PROTAC degrader, with pIC50 values of 8.37 and 7.12 against hsEH-H and msEH-H, respectively. PROTAC sEH degrader-2 induces targeted degradation of sEH via the ubiquitin-proteasome system, thereby completely blocking its dual functions as an epoxide hydrolase and a lipid phosphatase by bridging the short-branch exit of sEH with the CRBN E3 ubiquitin ligase. PROTAC sEH degrader-2 can be used in the research of neuroinflammation and 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 an orally active PROTAC-IMiD bifunctional protein degrader that selectively degrades BTK, IKZF1 and IKZF3. PROTAC BTK/IKZF1/3 Degrader-1 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, mediating ubiquitination and proteasome-dependent degradation of target proteins, with no obvious degrading effect on GSPT1. PROTAC BTK/IKZF1/3 Degrader-1 inhibits cancer cell proliferation, induces cancer cell apoptosis, and suppresses tumor growth. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of diffuse large B-cell lymphoma.
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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.
