| E1413 |
DEG-77
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DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
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| E6029 |
Lenalidomide hemihydrate
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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.
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| E1204 |
NVP-DKY709
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NVP-DKY709 is a potent IKZF2 inhibitor for the treatment of cancers.
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| S9832 |
CC-90009
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CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
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| E1847 |
GBD-9
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GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). This compound 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.
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| E1300 |
SJ6986
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SJ6986 is a CRBN modulator and specifically degrades GSPT1/2, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1.
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| E1937 |
PT-179
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PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. This compound 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.
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| E6651New |
HGC652
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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.
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| E1965 |
NST-628
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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.
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