Molecular Glues
Protein degradation agents based on the ubiquitin-proteasome pathway include a part of molecular glues. Molecular glues are a class of small molecule compounds that can induce or stabilize the interaction between proteins. If one of the protein is ubiquitin ligase, molecular glue can cause another protein to undergo ubiquitin modification and degradation through the proteasome pathway, which is similar to PROTAC. However, these molecules are classified as ligand for E3 ligase as functional molecules in subsequent classification. Older drugs, thalidomide, lenalidomide, and pomalidomide, together with CC-90009 and CC-92480 reported later all belong to this category.
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Molecular Glues Related Products (339)
Related Products (339)
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Related Compound Screening Libraries (1)
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NVP-DKY709
0 ImagesNVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2.
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WBC100
0 ImagesCat. No.: HY-145898CAS No.: 2095780-08-6Synonyms: 14-D-Valine-TPLWBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research.
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SJ6986
0 ImagesSJ6986 is a potent, selective and orally active GSPT1/2 Molecular Glue degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1.
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MRT-6160
0 ImagesSynonyms: VAV1 degrader-3MRT-6160 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). MRT-6160 reduces immune cell activation, immune cell proliferation and the production of various cytokines. MRT-6160 can be used for research of inflammatory or autoimmune disorder. MRT-6160 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc..
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Golcadomide
0 ImagesSynonyms: CC-99282Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).
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FPFT-2216
0 ImagesFPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.
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EN1033
0 ImagesEN1033 is a covalent immune regulatory transcription factor 5/8 (IRF5/8) molecular glue degrader. EN1033 degrades IRF5 in a proteasome-dependent manner. EN1033 engages and degrades IRF8 more robustly and rapidly. EN1033 covalently targets C28 and C223 to destabilize and degrade IRF5 and IRF8 respectively, thereby inhibiting their pro-inflammatory transcriptional activity. EN1033 serves as a promising tool for the study of autoimmune and inflammatory disorders.
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(R)-CR8
0 ImagesSynonyms: CR8, (R)-Isomer(R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
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XMU-MP-8
0 ImagesSynonyms: SKPer1XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma.
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Voclosporin
0 ImagesSynonyms: ISAtx-247Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor.
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BMS-986397
0 ImagesBMS-986397 is a potent, selective, and orally active cereblon-based molecular glue degrader of casein kinase 1α (CK1α). BMS-986397 induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells. BMS-986397 is a promising agent for the investigation of AML and high-risk myelodysplastic syndromes (HR-MDS).
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Rapamycin (Standard)
0 ImagesSynonyms: Sirolimus (Standard); AY-22989 (Standard); NSC 226080 (Standard)Rapamycin (Standard) (Sirolimus (Standard)) is the analytical standard of Rapamycin (HY-10219). This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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LC-04-045
0 ImagesCat. No.: HY-172162Purity: 99.56%LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia.
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NVS-STG2
0 ImagesNVS-STG2 is a molecular glue that targets STINGSTING by binding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models.
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Lenalidomide hemihydrate
0 ImagesSynonyms: CC-5013 hemihydrateLenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
