![Methyl (S)-2-(4-(4'-((4-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzyl)carbamoyl)-[1,1'-biphenyl]-4-yl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate](https://file.medchemexpress.com/product_pic/hy-153459.gif "Click to View Methyl (S)-2-(4-(4'-((4-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzyl)carbamoyl)-[1,1'-biphenyl]-4-yl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Product Detail")
![Boc‑2,6-Diazaspiro[3.3]heptane‑Py‑Ph‑acid](https://file.medchemexpress.com/product_pic/hy-189354.gif "Click to View Boc‑2,6-Diazaspiro[3.3]heptane‑Py‑Ph‑acid Product Detail")
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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
318 Results for "
Ternary complex
" in MedChemExpress (MCE) Product Catalog:
Products (318)
318 Results for "Ternary complex" in MCE Product Catalog:
Cat. No.: HY-159607
CAS No.: 2755761-78-3
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PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
Cat. No.: HY-L918
317 compounds
Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms.
Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases.
Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 317 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.
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IBG1 is a bivalent molecular glue degrader targeting BRD2/BRD4, with IC50 values of 12.8 nM and 462 nM, respectively, and an EC50 of 44 nM. By binding to the adjacent BD1 and BD2 bromodomains of BRD2 and BRD4, IBG1 stabilizes the ternary complex formed with DCAF16, thereby driving CRL-mediated ubiquitination and proteasomal degradation. IBG1 induces cancer cell apoptosis and inhibits cancer cell growth in a DCAF16-dependent manner, and downregulates MYC expression through DCAF16-independent BET bromodomain inhibition. IBG1 can be used in research of various cancers including prostate cancer .
Cat. No.: HY-159647
CAS No.: 2892065-45-9
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PLX-4545 is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PLX-4545 binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
Cat. No.: HY-161789
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PROTAC SARS-CoV-2 Mpro degrader-3 is a SARS-CoV-2 Mpro PROTAC degrader with a DC50 of 27 μM in HEK 293T cells. It also acts as an inhibitor of HCoV-229E, HCoV-OC43 and SARS-CoV-2 Mpro, with an IC50 of 0.748 μM and a Kd of 37 μM against SARS-CoV-2 Mpro. PROTAC SARS-CoV-2 Mpro degrader-3 forms a ternary complex with purified SARS-CoV-2 Mpro and VCB E3 ligase to induce intracellular protease degradation. It reduces coronavirus replication and can be used in research on coronavirus infections .
Cat. No.: HY-162280
CAS No.: 3034024-77-3
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PROTAC BTK Degrader-9 is a potent BTK PROTAC degrader with a DC50 of 1.29 nM (in Mino cells at 4 h). PROTAC BTK Degrader-9 induces the formation of a stable ternary complex with BTK and the CRBN E3 ubiquitin ligase, thereby mediating proteasomal degradation of BTK in a CRBN-dependent manner. PROTAC BTK Degrader-9 downregulates the RANKL-activated BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway. PROTAC BTK Degrader-9 alleviates alveolar bone resorption in periodontitis models of Mus musculus (house mouse). PROTAC BTK Degrader-9 can be used in research related to periodontitis .
Cat. No.: HY-162816
PROTAC HPK1 Degrader-3 is an orally active, PROTAC degrader that selectively targets HPK1, with a DC50 of 21.26 nM. PROTAC HPK1 Degrader-3 induces HPK1 degradation via the ubiquitin-proteasome system and forms a stable ternary complex with HPK1 and CRBN. It inhibits the SLP76 and NF-κB signaling pathways, enhances MAPK signal transduction, reverses the immunosuppressive factor-mediated inhibition of T cell cytokine secretion, and promotes the secretion of T cell immune cytokines. PROTAC HPK1 Degrader-3 suppresses tumor growth and enhances anti-PD-L1-mediated antitumor activity. It can be used in studies related to malignant tumors, such as colorectal cancer .
Cat. No.: HY-165426
CAS No.: 3031522-14-9
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HB-230 is a Transglutaminase-2 (TG2) (human IC50 = 4.9 μM) inhibitor and a selective fluorescent imaging probe for active TG2 localization. HB-230 modifies TG2 Cys277 to sustain the enzyme open conformation. HB-230 forms a ternary complex with TG2 and α2-macroglobulin, undergoes receptor-mediated endocytosis, and trafficks directly to lysosomes without early/late endosome fusion. HB-230 exhibits TG2 activity-dependent and α2-macroglobulin-dependent uptake. HB-230 can be used for the research of celiac disease, (Ex/Em = 649/665 nm) .
Cat. No.: HY-169369
CAS No.: 3109600-48-5
Synonyms: XJZ-06-462
TRAP-1 (XJZ-06-462) is a transcriptional activator of p53 (TRAP) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53 Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53 Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53 Y220C-carrying tumors .
Cat. No.: HY-172113
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma .
Cat. No.: HY-178496
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DDO3602 is a PARP1 HSPTAC (HSP90-mediated proteolysis-targeting chimera) degrader, with a DC50 of 490.3 nM against PARP1; its Kd values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively. DDO3602 induces the formation of an unnatural PARP1-HSP90 ternary complex, recruits E3 ubiquitin ligase, and promotes PARP1 degradation via the ubiquitin-proteasome pathway. DDO3602 induces G2/M cell cycle arrest, DNA damage, inhibits cell migration, and exhibits antiproliferative activity in breast cancer cells. DDO3602 can be used in breast cancer-related research .
Cat. No.: HY-179077
CAS No.: 2416130-49-7
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PROTAC 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 .
Cat. No.: HY-181154
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PROTAC SARS-CoV-2 Mpro degrader-5 is a SARS-CoV-2 main protease (Mpro) PROTAC. PROTAC SARS-CoV-2 Mpro degrader-5 engages CRBN E3 ubiquitin ligase to form a ternary complex with SARS-CoV-2 Mpro, induces K48-linked polyubiquitination of SARS-CoV-2 Mpro, and drives proteasome-dependent turnover of SARS-CoV-2 Mpro with a high selectivity index (CC50/DC50 > 10) in human embryonic kidney cells.PROTAC SARS-CoV-2 Mpro degrader-5 can be used for the research of COVID-19 .
Cat. No.: HY-181590
PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma .
Cat. No.: HY-181967
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PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma .
Cat. No.: HY-182275
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PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
Cat. No.: HY-182958
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Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)) .
Cat. No.: HY-168487
CAS No.: 2737222-94-3
PROTAC WDR5 degrader 1 is a heterobifunctional WDR5 PROTAC degrader with a DC50 value of 53 nM and a Kd value of 18 nM, exhibiting selective WDR5 degradation activity and cell permeability. PROTAC WDR5 degrader 1 induces proliferation defects in leukemia cells, with enhanced efficacy in cells overexpressing VHL. PROTAC WDR5 degrader 1 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-182980
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N-(8-Carboxyoctanoyl)-deacetyl BMS-202 is a target protein ligand-linker conjugate. N-(8-Carboxyoctanoyl)-deacetyl BMS-202 contains the target protein PD-1/PD-L1 ligand and a PROTAC linker. N-(8-Carboxyoctanoyl)-deacetyl BMS-202 can be used for the synthesis of PROTAC PD-L1 Degrader-3 (HY-182959) .
Cat. No.: HY-189354
CAS No.: 3138865-50-3
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Boc-2,6-Diazaspiro[3.3]heptane-Py-Ph-acid is a PROTAC linker. Boc-2,6-Diazaspiro[3.3]heptane-Py-Ph-acid can be used for the synthesis of PROTACs, such as LD5095 (HY-189352) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
