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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iDeg-6
0 ImagesCat. No.: HY-177785iDeg-6 is a molecular glue degrader that selectively targets IDO1, with a DC50 of 6.5 nM, an IC50 of 16 nM, and a Kd of 1.46 μM. iDeg-6 competes to bind the heme-binding site of apoprotein IDO1, promoting CRL2KLHDC3-mediated polyubiquitination of IDO1 and neddylation-modification-dependent proteasomal degradation. iDeg-6 reduces kynurenine production, abrogates the non-enzymatic pro-tumor migration function of IDO1, and inhibits tumor growth in immunodeficient mice. iDeg-6 can be used in studies of cancer, infection, and neurological diseases (such as melanoma).
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dRRM-1
0 ImagesCat. No.: HY-177779CAS No.: 253328-68-6dRRM-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.
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ZD-1-186
0 ImagesCat. No.: HY-180886ZD-1-186 is a non-degradative, covalent-dependent molecular glue that targets BCL6 and BRD9. ZD-1-186 inhibits the transcriptional output of MYC, relieves the repression of canonical BCL6 target loci (including CDKN1A (p21)), and mediates the selective recruitment of BRD9 to BCL6. ZD-1-186 can be used for research on diffuse large B-cell lymphoma.
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MEK-IN-10
0 ImagesCat. No.: HY-183674CAS No.: 3096958-11-8MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.
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BRD9 Degrader-3
0 ImagesCat. No.: HY-163810CAS No.: 3033018-77-5BRD9 Degrader-3 is a selective BRD9 BRD9 molecular glue degrader degrader. BRD9 Degrader-3 consists of a BRD9-binding ligand, a linker, and a warhead that promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of CRBN or VHL E3 ligases. BRD9 Degrader-3 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia.
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AR Degrader-3
0 ImagesCat. No.: HY-178938CAS No.: 1182011-65-9AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC).
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PLX-4104
0 ImagesCat. No.: HY-182912CAS No.: 2851986-77-9PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.
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GSPT1 degrader-17
0 ImagesCat. No.: HY-177766GSPT1 degrader-17 is a selective GSPT1 molecular glue degrader with a DC50 of 35 nM. GSPT1 degrader-17 induces GSPT1 degradation via the ubiquitin-proteasome system, which leads to G0/G1 phase cell cycle arrest and triggers apoptosis, thereby inhibiting the proliferation of leukemia cells. GSPT1 degrader-17 can be used in leukemia research.
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And1 degrader 1
0 ImagesCat. No.: HY-162896CAS No.: 3029132-46-2And1 degrader 1 is an acidic nucleoplasmic DNA-binding protein 1 (And1) molecular glue-like degrader. And1 degrader 1 binds to the WD40 domain of And1 in a 'V' conformation to induce And1 degradation via the ubiquitin-proteasome pathway. And1 degrader 1 exhibits antiproliferative activity via synthetic lethal interaction with a PARP1 inhibitor to inhibit proliferation of cancer cells. And1 degrader 1 can be used for the research of non-small cell lung cancer (NSCLC).
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CB039
0 ImagesCB039 is a RBM39 molecular glue degrader with an IC50 of 36.7 nM against HCT-116 cells. CB039 induces RBM39 degradation in a dose- and time-dependent manner. This process depends on the Cullin-RING E3 ubiquitin ligase complex (CRL) and proteasome, and promotes the recruitment of RBM39 to the DCAF15-DDB1 complex with an IC50 of 594 nM. CB039 causes abnormal RNA splicing, reduces CEP192 protein levels, induces G2/M phase cell cycle arrest and mitotic spindle disorder. CB039 can be used in studies on RBM39-targeted protein degradation and colorectal cancer-related mechanisms.
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IKZF2-degrader 5
0 ImagesCat. No.: HY-182945IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma.
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DHC-286
0 ImagesDHC-286 is a molecular glue degrader targeting GSPT1. DHC-286 recruits GSPT1 to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia.
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BCL6-IN-10
0 ImagesCat. No.: HY-177755CAS No.: 2230406-52-5BCL6-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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SB1349
0 ImagesCat. No.: HY-177782SB1349 is a potent Lin28 molecular glues degrader, with DC50 values of 1.594 µM and 0.777 µM for Lin28A and Lin28B, respectively. SB1349 induces proteasome-dependent degradation by directly binding and recruiting the E3 ubiquitin ligase RNF126. SB1349 can be used for the study of neuroblastoma.
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GSPT1 degrader-11
0 ImagesCat. No.: HY-177724GSPT1 degrader-11 is a CRBN-dependent molecular glue degrader targeting GSPT1, with a DC50 of 67.7 nM. GSPT1 degrader-11 induces CRBN-dependent degradation of GSPT1 via the ubiquitin-proteasome pathway. GSPT1 degrader-11 exhibits CRBN-dependent growth inhibitory activity in cancer cells. GSPT1 degrader-11 can be used for the research of triple-negative breast cancer.
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KAT2A degrader-1
0 ImagesCat. No.: HY-187168CAS No.: 2407654-72-0KAT2A degrader-1 is a molecular glue degrader targeting KAT2A, with a DC50 of 89 nM in Kelly cells. KAT2A degrader-1 recruits KAT2A to cereblon (CRBN) in a degron-independent manner, forms a ternary complex with KAT2A and CRBN, and drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-1 reduces the level of histone H3 lysine 9 acetylation (H3K9Ac). KAT2A degrader-1 induces antiproliferative effects in acute myeloid leukemia cells, while enhancing KAT2A-CRBN dimerization activity and eliminating the targeting effect on GSPT1. KAT2A degrader-1 can be used for research related to acute myeloid leukemia.
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BTX306
0 ImagesCat. No.: HY-177740CAS No.: 2230747-62-1BTX306 is a cereblon-targeting molecular glue degrader. BTX306 reduces myeloma cell viability and induces apoptosis. BTX306 overcomes myeloma cell resistance to Lenalidomide (HY-A0003) or Bortezomib (HY-10227). BTX306 is active against primary myeloma cells, and shows efficacy in vivo. BTX306 can be used for myeloma research.
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EST1140
0 ImagesCat. No.: HY-187458CAS No.: 3105892-11-0EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC50 values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.
