Molecular Glues

Molecular Glues製品

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Molecular Glues阻害剤 (3)
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新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1029	Lenalidomide (CC-5013)	Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) 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 promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Signal Transduct Target Ther, 2025, 10(1):29 Nat Commun, 2025, 16(1):3800 Cell Rep Med, 2025, S2666-3791(25)00102-8
S1567	Pomalidomide (CC-4047)	Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.	Nat Commun, 2025, 16(1):6631 Cell Rep Med, 2025, S2666-3791(25)00102-8 J Med Virol, 2025, 97(8):e70537
S1193	Thalidomide	Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.	Nat Genet, 2025, 57(10):2468-2481 Biomed Pharmacother, 2025, 184:117878 Nat Commun, 2024, 15(1):9195
S8760	Iberdomide (CC-220)	Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.	Cell Rep Med, 2025, S2666-3791(25)00102-8 J Med Virol, 2025, 97(8):e70537 Cancer Res, 2025, 10.1158/0008-5472.CAN-24-1136
S8975	Mezigdomide (CC-92480)	Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.	Nat Commun, 2024, 15(1):8885 Mol Cancer Ther, 2023, 22(5):659-666 Mol Cancer Ther, 2023, 22(5):659-666
E1427	MRT-2359	MRT-2359 is a potent degrader of GSPT1. It exhibits anti-tumor activity in non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells.
E6029	Lenalidomide hemihydrate	Lenalidomide hemihydrate (CC-5013 hemihydrate) is a potent inhibitor of TNF-alpha with a IC50 of 13 nM. It induces tyrosine phosphorylation of CD28 on T cells, which subsequently activates NF-κB. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), leading to the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex.
S9832	CC-90009	CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
E5871^New	VAV1 degrader-3	VAV1 degrader-3 (MRT-6160) is an orally active molecular glue degrader of VAV1 with a DC50 of 7 nM. It suppresses immune activation, proliferation, and cytokine production, inhibiting disease progression in inflammatory and autoimmune models like encephalomyelitis (EAE) and Collagen-induced arthritis (CIA).
E1937	PT-179	PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein.
E5854^New	XYD049	XYD049 (compound 7d) is a CRBN-based molecular glue targeting GSPT1 (DC50=19 nM), applicable for studying MYC-driven castration-resistant prostate cancer (CRPC). It demonstrates potent growth inhibition of 22Rv1 cells (IC50=7 nM) and exhibits in vivo antitumor activity. XYD049 downregulates CRPC-associated oncogenes (AR, AR-v7, PSA, c-Myc) in 22Rv1 cells. Structurally, it consists of: 1) a molecular glue linker (NH2-C5-NH-Boc), 2) a CRBN-recruiting E3 ligase ligand (Thalidomide 4-fluoride), and 3) a GSPT1-targeting moiety (GSPT1 ligand-1). The E3 ligase ligand-linker combination forms conjugate 158.
E1810	dCeMM1	dCeMM1 is a degrader of RBM39. dCeMM1 functions by altering the activity of the CRL4DCAF15 ligase, and also decreases RBM39 expression levels in wild-type KBM7 cells.
E6029	Lenalidomide hemihydrate	Lenalidomide hemihydrate (CC-5013 hemihydrate) is a potent inhibitor of TNF-alpha with a IC50 of 13 nM. It induces tyrosine phosphorylation of CD28 on T cells, which subsequently activates NF-κB. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), leading to the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex.
S9832	CC-90009	CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
E1937	PT-179	PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein.
S8975	Mezigdomide (CC-92480)	Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.	Nat Commun, 2024, 15(1):8885 Mol Cancer Ther, 2023, 22(5):659-666 Mol Cancer Ther, 2023, 22(5):659-666
E5871^New	VAV1 degrader-3	VAV1 degrader-3 (MRT-6160) is an orally active molecular glue degrader of VAV1 with a DC50 of 7 nM. It suppresses immune activation, proliferation, and cytokine production, inhibiting disease progression in inflammatory and autoimmune models like encephalomyelitis (EAE) and Collagen-induced arthritis (CIA).
E5854^New	XYD049	XYD049 (compound 7d) is a CRBN-based molecular glue targeting GSPT1 (DC50=19 nM), applicable for studying MYC-driven castration-resistant prostate cancer (CRPC). It demonstrates potent growth inhibition of 22Rv1 cells (IC50=7 nM) and exhibits in vivo antitumor activity. XYD049 downregulates CRPC-associated oncogenes (AR, AR-v7, PSA, c-Myc) in 22Rv1 cells. Structurally, it consists of: 1) a molecular glue linker (NH2-C5-NH-Boc), 2) a CRBN-recruiting E3 ligase ligand (Thalidomide 4-fluoride), and 3) a GSPT1-targeting moiety (GSPT1 ligand-1). The E3 ligase ligand-linker combination forms conjugate 158.