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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CDK2 degrader 9
0 ImagesCat. No.: HY-181620CDK2 degrader 9 (compound 1) is a CDK2-targeting Molecular Glue with selectivity for GSPT1 and CDK1. CDK2 degrader 9 promotes the ubiquitination and degradation of CDK2 via the ubiquitin ligase pathway. CDK2 degrader 9 is applicable to research related to cancer, solid tumors and hematologic malignancies.
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PIN1 degrader-3
0 ImagesCat. No.: HY-179577CAS No.: 3101950-55-1PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50=4.65 nM) molecular glue degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability. PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer.
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AG6033
0 ImagesCat. No.: HY-143435CAS No.: 329706-62-9AG6033 is a CRBN-dependent molecular glue degrader targeting GSPT1 (DC50 of 2.5 μM) and IKZF1. AG6033 induces degradation of GSPT1 via π-π stacking and hydrogen bonding with CRBN in a partially CRBN-dependent manner, decreases IKZF1 levels, and promotes degradation of CRBN substrates. AG6033 induces apoptosis in lung adenocarcinoma cells. AG6033 can be used for the research of lung cancer.
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HRZ-01-082-5
0 ImagesCat. No.: HY-175875CAS No.: 3090685-19-8HRZ-01-082-5 is an analog of Glutarimide (HY-I0466). HRZ-01-082-5 is a dual-functional molecular glue degrader of SALL4 and OSR1 with a DC50 4.8 nM for OSR1. HRZ-01-082-5 significantly induced SALL4 and OSR1 degradation through CRBN. HRZ-01-082-5 can be used for heart and urogenital development, as well as cancers research.
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MG-Lin3
0 ImagesCat. No.: HY-177733MG-Lin3 is a Lin28 molecular glue degrader. MG-Lin3 recruits the E3 ubiquitin ligase RNF126 to form a ternary complex, induces the degradation of Lin28 via the ubiquitin-proteasome pathway, and restores the levels of mature let-7 miRNA. MG-Lin3 can be used in research on ovarian cancer, ovarian teratocarcinoma, and uterine cancer.
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M12
0 ImagesCat. No.: HY-189123CAS No.: 724429-20-3M12 is a DCAF11-dependent molecular glue degrader activated by glutathionylation, which induces CRL4DCAF11-mediated degradation of DDX18. M12 is a precursor compound that requires metabolic activation: it is conjugated with glutathione (GSH) under the catalysis of glutathione S-transferase (GST) to form GSH-M12, which interacts with DCAF11 and promotes the recruitment of DDX18. M12 is applicable for studies on targeted protein degradation and DCAF11-dependent molecular glue mechanisms.
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IKZF3 degrader 1
0 ImagesCat. No.: HY-169077Purity: 99.19%IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3.
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TBK1 degrader-4
0 ImagesCat. No.: HY-176255TBK1 degrader-4 (Compound 30) is a molecular glue degrader targeting TBK1. TBK1 degrader-4 effectively inhibits cyst growth, alleviates inflammation, and reduces the levels of pro-inflammatory factors such as Ccl2, IFNβ, and IL-6. TBK1 degrader-4 is promising for research of autosomal dominant polycystic kidney disease (ADPKD).
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GSPT1 degrader-1
0 ImagesCat. No.: HY-155552CAS No.: 3037491-05-4GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G0/G1 phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research.
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Galeterone hydrochloride
0 ImagesCat. No.: HY-70006ACAS No.: 1239339-17-3Synonyms: TOK-001 hydrochloride; VN-124-1 hydrochlorideGaleterone (TOK-001) hydrochloride is a potent, 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. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].
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Pomalidomide-β-D-glucose
0 ImagesCat. No.: HY-189288CAS No.: 2894135-13-6Pomalidomide-β-D-glucose is an orally active Molecular glue degrader of IKZF1 and CK1α. Pomalidomide-β-D-glucose forms a ternary complex with CRBN and substrate proteins, inducing ubiquitination and proteasomal degradation of IKZF1 and CK1α. Pomalidomide-β-D-glucose undergoes GLUT1-mediated cellular uptake. Pomalidomide-β-D-glucose can be used for research on multiple myeloma.
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eEF2K degrader-2
0 ImagesCat. No.: HY-177720CAS No.: 1044797-96-7eEF2K degrader-2 (Compound C1) is a molecular glucose degrading agent that targets the eEF2K protein. eEF2K degrader-2 can significantly inhibit the proliferation, migration, invasion and induce apoptosis of triple negative breast cancer (TNBC) cells. eEF2K degrader-2 has no obvious organ toxicity or pathological damage. eEF2K degrader-2 can be used in the research of cancer such as breast cancer.
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JP-2-249
0 ImagesCat. No.: HY-161883CAS No.: 3036530-41-0
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TEAD degrader-1
0 ImagesCat. No.: HY-184179CAS No.: 3103984-17-1TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC50 of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer.
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IBA-11
0 ImagesCat. No.: HY-182800IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia.
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DIX-01
0 ImagesCat. No.: HY-180836DIX-01 is a CRBN-recruiting molecular glue and cytotoxic agent targeting GSPT1, with an EC50 of 173 nM against human GSPT1. DIX-01 drives proteasomal degradation of GSPT1, IKZF1 and IKZF3, and induces cytotoxicity in cancer cells. DIX-01 inhibits tumor growth in a zebrafish xenograft model and can be used for research on acute myeloid leukemia and prostate cancer.
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GSPT1 degrader-2
0 ImagesCat. No.: HY-156747CAS No.: 2803879-60-7GSPT1 degrader-2 is an orally active GSPT1 molecular glue degrader that promotes the degradation of intracellular GSPT1 protein, with DC50 values of 3 nM and 22 nM in NCI-H1155 and ABC-1 cells with high N-Myc expression, respectively. GSPT1 degrader-2 can be used in the research of N-Myc-driven cancers, such as lung cancer.
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ABT-002
0 ImagesCat. No.: HY-175283CAS No.: 2438239-83-7ABT-002 is a molecular glue degrader targeting GSPT1 and NEK7. ABT-002 is the active metabolite of ABS-752 (HY-W599279). ABT-002 is promising for research of hepatocellular carcinoma (HCC).
