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Molecular Glues製品

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S1029 CC-5013 (Lenalidomide) 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
Lenalidomide-S102901W0320121120.gif
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
Pomalidomide-S156701X0120110822.gif
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
Thalidomide-S119301W0620170505.gif
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.
E1204 NVP-DKY709 NVP-DKY709 is a potent IKZF2 inhibitor for the treatment of cancers.
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.
E1847 GBD-9 GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival.
E5871New 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).
E1300 SJ6986 SJ6986 is a CRBN modulator and specifically degrades GSPT1/2, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1.
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.
E6651New HGC652 HGC652 is a TRIM21-dependent molecular glue degrader that binds the E3 ubiquitin ligase TRIM21 (Kd ≈ 0.06 µM) to induce a TRIM21–NUP98 ternary complex, driving the ubiquitination and selective degradation of nuclear pore complex proteins like NUP155, leading to nuclear pore collapse and cancer cell death.
E5854New 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.
E1965 NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.
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
E1847 GBD-9 GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival.
E1965 NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.
E5871New 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).
E6651New HGC652 HGC652 is a TRIM21-dependent molecular glue degrader that binds the E3 ubiquitin ligase TRIM21 (Kd ≈ 0.06 µM) to induce a TRIM21–NUP98 ternary complex, driving the ubiquitination and selective degradation of nuclear pore complex proteins like NUP155, leading to nuclear pore collapse and cancer cell death.
E5854New 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.
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