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 (372)
Related Products (372)
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Related Compound Screening Libraries (1)
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Lenalidomide hydrochloride
0 ImagesCat. No.: HY-A0003ACAS No.: 1243329-97-6Synonyms: CC-5013 hydrochlorideLenalidomide hydrochloride (CC-5013 hydrochloride) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide hydrochloride induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide hydrochloride promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide hydrochloride can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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Cyclosporin A-d12
0 ImagesCat. No.: HY-B0579S5Synonyms: Cyclosporine A-d12; Ciclosporin A-d12; CsA-d12Cyclosporin A-d12 (Cyclosporine A-d12) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.
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NEO-811
0 ImagesCat. No.: HY-183117CAS No.: 3084635-77-5NEO-811 is a selective and orally active ARNT (HIF-1β) molecular glue degrader. NEO-811 is mediated by CRL4-CRBN E3 ligase for ARNT degradation. NEO-811 can be used for the study of clear cell renal cell carcinoma (ccRCC).
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AMX-883
0 ImagesCat. No.: HY-182766CAS No.: 3102636-19-8AMX-883 a selective and orally active BRD9 molecular glue degrader that drives differentiation in acute myeloid leukaemia. AMX-883 shows selectivity over all other bromodomain containing proteins and proteome wide. AMX-883 does not employ the commonly used E3 ligases (cereblon, VHL) but instead drives degradation via DCAF16 as a targeted glue. AMX-883 can be used for the study of acute myeloid leukaemia (AML).
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XYD113
0 ImagesCat. No.: HY-184896CAS No.: 3032314-99-8XYD113 is an orally active, selective GSPT1 Molecular glue degrader. XYD113 promotes the formation of the CRBN-GSPT1 ternary complex and mediates GSPT1 degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. XYD113 downregulates genes associated with the occurrence and progression of prostate cancer (c-Myc, AR, AR-V7, KLK3, KLK2, TMPRSS2). XYD113 exhibits anticancer activity against prostate cancer. XYD113 can be used in the research of prostate cancer.
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NVP-KFA115
0 ImagesCat. No.: HY-189390CAS No.: 2408998-17-2
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KT-333 diammonium
0 ImagesCat. No.: HY-156730BCAS No.: 2502186-80-1KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).
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Avadomide hydrochloride
0 ImagesCat. No.: HY-100507ACAS No.: 1398053-45-6Synonyms: CC 122 hydrochlorideAvadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.
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GSPT1 degrader-4
0 ImagesCat. No.: HY-162533CAS No.: 3034764-32-1
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GSPT1 degrader-16
0 ImagesCat. No.: HY-177765CAS No.: 3060504-68-6GSPT1 degrader-16 (Compound Lib-B-18J) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-16 shows inhibitory effect to RS4;11, Molt4, and MM.1S cells with IC50 values of 0.002, 0.26 and 0.37 μM. GSPT1 degrader-16 can be used for the research of cancer, such as acute lymphoblastic leukemi.
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IKZF2-degrader 3
0 ImagesCat. No.: HY-177754CAS No.: 2983841-46-7IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM.
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IKZF-IN-1
0 ImagesCat. No.: HY-170518IKZF-IN-1 is a molecular glue and an IKZF protein degrader that mediates the degradation of IKZF1/IKZF2/IKZF3/IKZF4 proteins. IKZF-IN-1 promotes the ubiquitination of target proteins via the CUL4‑CRBN E3 ubiquitin ligase complex, thereby triggering the degradation of target proteins. IKZF-IN-1 can be used in cancer-related research.
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TD-522
0 ImagesCat. No.: HY-177750CAS No.: 2417647-40-4TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research.
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NEK7 degrader-3
0 ImagesCat. No.: HY-185311CAS No.: 3119435-52-5NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
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SMARCA2/4 degrader-1
0 ImagesCat. No.: HY-175756CAS No.: 2901804-87-1SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer.
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Antitumor agent-100 hydrochloride
0 ImagesCat. No.: HY-153802ACAS No.: 2841750-53-4Antitumor agent-100 hydrochloride is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 hydrochloride binds to the catalytic pocket of PDE3A, extends hydrophobic groups to mediate the hydrophobic interaction between PDE3A and SLFN12, and stabilizes the PDE3A-SLFN12 complex. Antitumor agent-100 hydrochloride induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 hydrochloride can be used for the research of cervical cancer.
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TBE56
0 ImagesCat. No.: HY-17655TBE56, a molecular glue, is a BACH1 degrader, with an EC50 of 44 nM. TBE56 is a weak NRF2 inducer and the biotinylated TBE31. TBE56 interacts and promotes the degradation of BACH1 via a mechanism involving the E3 ligase FBX022. TBE56 reduces intracellular Fe2+ accumulation, ROS generation, and malondialdehyde (MDA) content, while increasing GSH/GSSG ratio and upregulating GPX4 in Prominin-2-overexpressed BMSCs. TBE56 significantly ameliorates intervertebral disc degeneration (IVDD) in puncture-induced SD rat IVDD model. TBE56 can be used for the study of intervertebral disc degeneration (IVDD).
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YSA64
0 ImagesCat. No.: HY-183755Purity: 98.06%YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma.
