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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
38 Results for "
molecular glue interactions
" in MedChemExpress (MCE) Product Catalog:
Products (38)
38 Results for "molecular glue interactions" in MCE Product Catalog:
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2 Cited Publications
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HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
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1 Cited Publications
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dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
Cat. No.: HY-170430
CAS No.: 3055558-98-7
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HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death .
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HB007 is a SUMO1 molecular glue degrader targeting CAPRIN1 and FBXO42. HB007 selectively binds CAPRIN1 to induce CAPRIN1-FBXO42 interaction, recruits SUMO1 to the CAPRIN1-CUL1-FBXO42 E3 ligase complex, and drives SUMO1 ubiquitination and degradation without affecting SUMO2/3. HB007 induces TCF4 deSUMOylation and proteasomal degradation to inhibit StarD7 transcriptional activity, reduces StarD7 mRNA and protein levels, and triggers ER stress and ROS production. HB007 can be used for the research of brain cancer, breast cancer, colon cancer, lung cancer .
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HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .
Cat. No.: HY-153193
CAS No.: 2765539-59-9
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LSN3160440 is an allosteric modulator of GLP-1R, which acts as a protein–protein interaction (PPI) stabilizer or molecular glue to assist in the adhesion of inactive GLP-1 (9-36) NH2 on GLP-1R .
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NRX-1933 is a molecular glue (molecular glue) that enhances the interaction between β-catenin and β-TrCP. NRX-1933 promotes the ubiquitination and subsequent degradation of mutant β-catenin. NRX-1933 can be applied to tumor research involving aberrant activation of the Wnt/β-catenin signaling pathway .
Cat. No.: HY-W133627
CAS No.: 118719-16-7
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dCeMM1 is a molecular glue degrader that targets RBM39. dCeMM1 serves as a positive control for the screening of DCAF15-dependent molecular glue degraders. dCeMM1 promotes the DCAF15-RBM39 interaction, thereby recruiting RBM39 to the CRL4 DCAF15 E3 ubiquitin ligase complex, inducing ubiquitination and subsequent proteasomal degradation of RBM39. Meanwhile, dCeMM1 stabilizes DCAF15 by mediating neo-substrate recruitment to protect DCAF15 from autodegradation. dCeMM1 reduces the viability of leukemia cells in a neddylation-dependent and proteasome-dependent manner, and can be applied in leukemia-related research .
Cat. No.: HY-169325
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(S)-ACE‑OH is the active metabolite of Acepromazine (HY-B1506), acting as a molecular glue degrader. (S)-ACE-OH induces functional interaction between TRIM21 and NUP98, promoting protein ubiquitination and degradation of TRIM21 at the nuclear pore complex. (S)-ACE-OH triggers nucleocytoplasmic transport disorder and exerts interferon-potentiated cytotoxic effects on certain cancer cells. (S)-ACE-OH can be used in cancer-related research .
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dCeMM4 is a Cyclin K Molecular glue degrader. dCeMM4 mediates the direct interaction between CDK12:cyclin K and the CRL4B ligase complex, thereby driving the ubiquitination and proteasomal degradation of Cyclin K. dCeMM4 induces Apoptosis without cell cycle phase-specific arrest. dCeMM4 exhibits synergistic activity with DNA damage inducers, and a correlation exists between Cyclin K degradation and cellular sensitivity. dCeMM4 can be used in studies related to T-cell malignancies .
MMH1 is a novel BRD4 molecular glue degrader. MMH1 functions by recruiting the CUL4 DCAF16 ligase to the second bromodomain of BRD4 (BRD4 BD2). MMH1 binds to the JQ1-binding site of BRD4 BD2, acts as a template to covalently modify Cys58 of DCAF16, stabilizes the BRD4-DCAF16 ternary complex, and thereby promotes BRD4 degradation via the CRL4DCAF16 ubiquitin ligase pathway. Using BRD4 BD2 as a structural template, MMH1 covalently modifies Cys87 of GAK and induces the GAK-BRD4 BD2 interaction. Through its covalent mechanism, MMH1 exhibits sustained BRD4 degradation activity, and shows selective degradation activity for BRD4 BD2 over BRD4 BD1 .
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dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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NRX-103094 is a Molecular glue and β-catenin/β-TrCP interaction enhancer, with an EC50 of 62 nM for the binding of pSer33/S37A β-catenin peptide to recombinant β-TrCP/Skp1 complex. NRX-103094 shows selectivity for Ser37 phosphorylation-deficient β-catenin, and has no effect on wild-type doubly phosphorylated β-catenin or other β-TrCP substrates. NRX-103094 can be used in research related to colorectal cancer and ovarian endometrioid adenocarcinoma .
Cat. No.: HY-169905
CAS No.: 271798-59-5
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GR-14-3-3 stabilizer-1 is a molecular glue stabilizer for the protein-protein interaction between 14‑3‑3 and glucocorticoid receptor (GR), and functions by stabilizing the GR‑14‑3‑3 protein-protein interaction. GR-14-3-3 stabilizer-1 is applicable to research related to diseases such as tumors .
Cat. No.: HY-177742
CAS No.: 2251753-65-6
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LXH-3-71 is a PHGDH degrader. LXH-3-71 acts as a molecular glue to enhance the interaction of the PHGDH-DDB1-CRL E3 ligase complex, triggering ubiquitination and proteasomal degradation of PHGDH. LXH-3-71 regulates the stemness of colorectal cancer cells and inhibits tumor proliferation and colony formation. LXH-3-71 can be used in the research of colorectal cancer .
Cat. No.: HY-175453
CAS No.: 3050683-03-6
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MRT-23227 is a CRBN-recruiting molecular glue degrader targeting VAV1. MRT-23227 binds to the tryptophan triad pocket of CRBN, forms a ternary complex with the SH3c domain of VAV1, and induces proteasomal degradation of VAV1 through hydrogen-bond interactions between CRBN residues and the RT loop and side chains of VAV1. MRT-23227 can be used in the research of T-cell leukemia and lymphoma .
Cat. No.: HY-W1005067
CAS No.: 2191110-79-7
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EN171 is a covalent 14-3-3σ molecular glue ligand that sequesters neonuclear substrates, including BRD4 and BLC6, into the cytoplasm by recruiting 14-3-3σ. EN171 covalently targets C38 and C96 on 14-3-3 to enhance the interaction between 14-3-3 and ERα, YAP, and TAZ (with EC50 values of 9 μM for human ERα, 45 μM for YAP, and 107 μM for TAZ). EN171 inhibits the transcriptional activity of estrogen receptors and the Hippo pathway in breast cancer cells. EN171 can be used in studies related to breast cancer .
Cat. No.: HY-177779
CAS No.: 253328-68-6
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dRRM-1 is a DCAF15-dependent RBM39/RBM23 molecular glue degrader. dRRM-1 stabilizes the interaction between DCAF15 and the novel substrates RBM39 and RBM23, thereby triggering their ubiquitination and degradation. dRRM-1 can be applied in research related to cancer .
Cat. No.: HY-150641
CAS No.: 3031561-92-6
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CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
Cat. No.: HY-177755
CAS No.: 2230406-52-5
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BCL6-IN-10 is a molecular glue inhibitor targeting the BCL6 BTB domain with an IC50 of 4 nM. BCL6-IN-10 blocks the interaction between BCL6 and transcriptional co-repressors, and induces partial degradation of BCL6 via the ubiquitin-proteasome pathway, thereby de-repressing BCL6 target genes and inhibiting cancer cell proliferation. BCL6-IN-10 can be used in the research of diffuse large B-cell lymphoma .
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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
