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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MyD88 degrader-1
0 ImagesCat. No.: HY-184470MyD88 degrader-1 is an orally active molecular glue degrader targeting MyD88, with a DC50 of 0.74 μM, and exhibits potent anti-inflammatory activity. MyD88 degrader-1 promotes ubiquitination and proteasomal degradation of MyD88, blocks the activation of the NF-κB signaling pathway, and downregulates the transcription of pro-inflammatory genes such as IL-6 and IL-1β. MyD88 degrader-1 alleviates symptoms in acute lung injury models. MyD88 degrader-1 can be used in studies related to acute lung injury.
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TRIM21 ligand-1
0 ImagesCat. No.: HY-186250CAS No.: 3055559-33-3
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TYMJ-01
0 ImagesCat. No.: HY-181506CAS No.: 3109321-90-3TYMJ-01 is a fluorescent probe and eEF2K degrader. TYMJ-01 induces dose-dependent and specific degradation of eEF2K via the ubiquitin-proteasome pathway, with a DC50 of 82 nM. TYMJ-01 inhibits the proliferation, migration and invasion of triple-negative breast cancer cells. TYMJ-01 enables dynamic fluorescent imaging of eEF2K degradation in triple-negative breast cancer cells; it enhances the anti-tumor activity of Paclitaxel (HY-B0015). TYMJ-01 can be used for the research of triple-negative breast cancer.
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LCK degrader-3
0 ImagesCat. No.: HY-180928CAS No.: 3095032-59-7LCK degrader-3 (Compound 20) is a CRBN-based LCK molecular glue degrader. LCK degrader-3 can be used in the research of acute lymphoblastic leukemia.
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GPX4-IN-20
0 ImagesCat. No.: HY-178389GPX4-IN-20, a Arctigenin (HY-N0035) derived, is a GPX4& molecular gluedegrader. GPX4-IN-20 induces ferroptosis by increasing lipid ROS levels and suppressing GSH levels. GPX4-IN-20 reduces the protein expression and enzyme activity of GPX4 in a dose-dependent manner without affecting other ferroptosis-related proteins. GPX4-IN-20 induces ubiquitination-dependent proteasomal degradation of GPX4. GPX4-IN-20 also increases the level of malondialdehyde (MDA) in HCT-116 cells. GPX4-IN-20 can be used for the research of colorectal cancer.
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MG-Lin2
0 ImagesCat. No.: HY-177732MG-Lin2 is a Lin28 molecular glue degrader. It induces the formation of a ternary complex between Lin28 and the E3 ubiquitin ligase RNF126, mediates the degradation of Lin28 via the ubiquitin-proteasome pathway, and restores the abundance and function of mature let-7 miRNA. MG-Lin2 can be used in studies of ovarian cancer and choriocarcinoma.
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VNPP433-3β dihydrochloride
0 ImagesCat. No.: HY-160777ACAS No.: 3026905-92-7Synonyms: Galeterone 3β-imidazole dihydrochlorideVNPP433-3β (Galeterone 3β-imidazole) dihydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
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AURKA-IN-4
0 ImagesAURKA-IN-4 is a Capsaicin (HY-10448)-derived molecular glue targeting AURKA-PHB2, and acts as an inhibitor of Aurora kinase A (AURKA) and PHB2. AURKA-IN-4 binds to the active site of AURKA and the inhibitory pocket of PHB2, inhibits AURKA-dependent mitophagy, and increases mitochondrial mass in cancer cells overexpressing AURKA. AURKA-IN-4 can be used in the research of breast cancer.
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Lenalidomide-13C5,15N
0 ImagesCat. No.: HY-A0003S2Synonyms: CC-5013-13C5,15NLenalidomide-13C5,15N (CC-5013-13C5,15N) is the 13C, 15N-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) 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 induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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Cyclosporin A-KLH
0 ImagesCat. No.: HY-NP194BCyclosporin A-KLH is a conjugate of Cyclosporin A (HY-B0579) and KLH. Cyclosporin A is an immunosuppressant which binds to the cyclophilin .
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LCK degrader-2
0 ImagesCat. No.: HY-175463CAS No.: 3095032-50-8LCK degrader-2 is a selective CRBN-dependent molecular glue degrader targeting LCK. LCK degrader-2 induces the proximity effect between LCK and CRBN, stabilizes the CRBN-LCK ternary complex, and triggers the ubiquitination and degradation of LCK. LCK degrader-2 can be used for the research of acute lymphoblastic leukemia.
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(R,R)-dWIZ-1
0 ImagesCat. No.: HY-169761ACAS No.: 2654005-60-2(R,R)-dWIZ-1 is the (R,R) enantiomer of dWIZ-1 (HY-159098). dWIZ-1 is a potent WIZ molecular glue degrader. (R,R)-dWIZ-1 can be used in studies related to sickle cell disease and β-thalassemia.
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BRD9 Degrader-2
0 ImagesCat. No.: HY-163809CAS No.: 3033018-68-4BRD9 Degrader-2 is a selective BRD9 molecular glue degrader. BRD9 Degrader-2 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-2 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia.
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BRD4 degrader-7
0 ImagesCat. No.: HY-183077BRD4 degrader-7 (Compound ZZ1) is a CTLH-dependent BRD4 degrader and c-Glue with a DC50 of 489 nM. BRD4 degrader-7 converts to a sulfinic acid derivative inside cells, interacts with the basic pocket of YPEL5, mediates the bridging of BRD4 BD1 to the YPEL5 subunit of the CTLH E3 ubiquitin ligase, and thereby promotes the formation of a ternary complex. BRD4 degrader-7 can be used in research on Ewing's sarcoma and leukemia.
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GPX4 degrader-2
0 ImagesCat. No.: HY-181656GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer.
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BRD4 degrader-2
0 ImagesCat. No.: HY-163639CAS No.: 3036530-43-2
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AR Degrader-1
0 ImagesCat. No.: HY-163641AR Degrader-1 is a molecular glue degrader targeting the androgen receptor (AR). AR Degrader-1 induces androgen receptor degradation by recruiting the DCAF16 E3 ligase substrate receptor, thereby triggering ubiquitination and proteasomal degradation. AR Degrader-1 exhibits relatively selective degradation of the androgen receptor in prostate cancer cells, reducing the levels of only a small number of other proteins. AR Degrader-1 can be used in studies related to prostate cancer.
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IBA-12
0 ImagesCat. No.: HY-182799IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research.
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MS1-96
0 ImagesCat. No.: HY-179558MS1-96 is an orally active PD-L1 (programmed death-ligand 1) molecular glue degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer.
