DC74482 |
CC-3240
Featured
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CC-3240 is an optimized molecular glue degrader derived from CC-8977, demonstrating high-affinity binding to CaMKK2 (IC50 = 9 nM) and potent degradation efficacy (DC50 = 100 nM in THP1 cells, Dmax = 92%). This novel compound effectively hijacks the ubiquitin-proteasome system to induce targeted CaMKK2 depletion, offering a superior pharmacological approach over traditional kinase inhibition. |
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DC74572 |
DEG-77
Featured
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DEG-77 is a cereblon-dependent degrader targeting IKZF2 and casein kinase 1α (CK1α). It effectively blocks cell growth and delays leukemia progression in both murine and human acute myeloid leukemia (AML) mouse models. |
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DC60567 |
dCeMM1
Featured
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dCeMM1 is a molecular glue degrader targeting RBM39. It functions by redirecting the activity of the CRL4DCAF15 ligase, leading to a reduction in RBM39 levels in WT KBM7 cells. |
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DC60572 |
NST-628
Featured
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NST-628 is a brain-penetrant molecular glue targeting the MAPK pathway, effectively inhibiting RAF phosphorylation and MEK activation. By binding to RAF, it disrupts the formation of BRAF-CRAF and BRAF-ARAF heterodimers, thereby blocking the RAS-MAPK signaling cascade. NST-628 exhibits potent anti-tumor activity in RAS- and RAF-driven cancers, demonstrating significant efficacy in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumor models. |
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DC60617 |
dWIZ-1
Featured
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dWIZ-1 is a first-in-class molecular glue degrader that specifically targets the WIZ transcription factor for proteasomal degradation, leading to potent induction of fetal hemoglobin (HbF) in erythroblasts. This novel compound functions by enhancing the interaction between CRBN and WIZ, demonstrating an EC50 of 547 nM for CRBN-WIZ complex formation. |
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DC60624 |
OPB-171775
Featured
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OPB-171775 represents a breakthrough in GIST treatment as a first-in-class, non-tyrosine kinase inhibitor (non-TKI) compound that demonstrates potent antitumor activity independent of KIT mutation status. Unlike conventional TKIs that target oncogenic kinases, OPB-171775 operates through an innovative mechanism by orchestrating a protein-protein interaction between phosphodiesterase 3A (PDE3A) and Schlafen 12 (SLFN12). |
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DC60634 |
LL-K12-18
Featured
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LL-K12-18 is a highly potent dual-site molecular glue that induces the formation of the CDK12-DDB1 complex, exhibiting an EC50 of 0.37 nM. It demonstrates 80-fold greater potency than SR-4835 in MDA-MB-231 cells and a remarkable 307-fold increase in potency (EC50 = 0.03 nM) in MDA-MB-468 cells, while its degradation efficiency (DC50 = 0.38 nM) is 50-fold enhanced. |
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DC66608 |
BMS-986397
Featured
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DC66609 |
PLX-4545
Featured
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PLX-4545 is an orally bioavailable molecular glue degrader that hijacks the cereblon E3 ubiquitin ligase complex to selectively target IKZF2 (Helios), a zinc finger transcription factor critical for regulatory T cell (Treg) function. By inducing proteasomal degradation of IKZF2, PLX-4545 disrupts Treg stability and reprograms these immunosuppressive cells into pro-inflammatory effector-like T cells, effectively shifting the tumor microenvironment toward immune activation. |
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DC60654 |
CDO1 degrader-1
Featured
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CDO1 Degrader-1 (Compound 8) is a molecular glue that targets cysteine dioxygenase (CDO1) for degradation. |
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DC60676 |
MRT6160
Featured
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MRT-6160 represents a groundbreaking molecular glue degrader designed to selectively target VAV1, achieving its proteasomal degradation with a DC50 value of 7 nM. This innovative compound showcases its unique mechanism and therapeutic potential. |
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DC67325 |
(S)-ACE-OH
Featured
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(S)-ACE-OH is a molecular glue exhibiting anticancer properties by facilitating the degradation of nucleoporins and disrupting nucleocytoplasmic transport. It achieves this by inducing an interaction between the E3 ubiquitin ligase TRIM21 and the nucleoporin NUP98. |
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DC67326 |
LYG-409
Featured
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LYG-409 is an orally active degrader of GSPT1, demonstrating significant efficacy against acute myeloid leukemia and prostate cancer in vivo, with tumor growth inhibition (TGI) rates of 94.34% and 104.49%, respectively. In vitro, LYG-409 effectively inhibits KG-1 cells by degrading GSPT1, exhibiting an IC50 of 9.50 nM and a DC50 of 7.87 nM. |
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DC67327 |
Lenalidomide hemihydrate
Featured
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Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of thalidomide, functions as a molecular glue and is an orally active immunomodulator. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), facilitating the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex. Lenalidomide hemihydrate specifically inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes the release of IL-2 from T cells.
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DC67328 |
ALV1
Featured
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ALV1 is a molecular glue degrader targeting Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. It binds to CRBN with an IC50 of 0.55 µM and induces CRBN-Helios dimerization. ALV1 is a valuable tool for studying the properties and functions of regulatory T cells (Treg cells). |
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DC67329 |
TMX1
Featured
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TMX1 is a covalent molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4BD2 domain, resulting in the degradation of BRD4. |
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DC67330 |
MYC degrader 1
Featured
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MYC degrader 1 (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, with significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. |
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DC67331 |
MMH2
Featured
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MMH2 is a novel BRD4 molecular glue degrader that operates by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). |
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DC67332 |
GBD-9
Featured
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GBD-9 is a dual-mechanism degrader that effectively targets BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It functions both as a PROTAC molecule to degrade BTK and as a molecular glue to induce GSPT1 degradation. GBD-9 demonstrates potent inhibition of cancer cell growth. |
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DC67333 |
MYC degrader 1 TFA
Featured
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MYC degrader 1 TFA (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, exhibiting significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. |
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DC67334 |
Tz-Thalidomide
Featured
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Tz-Thalidomide is a tetrazine-functionalized derivative of thalidomide (HY-14658) designed for targeted protein degradation applications. This bifunctional molecule serves as an E3 ligase ligand while maintaining binding affinity for BRD4, with IC50 values of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). |
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DC67335 |
MMH1
Featured
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MMH1 is a first-in-class molecular glue degrader that specifically targets the second bromodomain of BRD4 (BRD4BD2) through an innovative mechanism of action. By simultaneously engaging both BRD4BD2 and the CUL4-DCAF16 E3 ubiquitin ligase complex, MMH1 induces targeted protein degradation with exceptional specificity. |
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DC67336 |
HbF inducer 2
Featured
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HbF inducer 2 is an orally bioavailable molecular glue that selectively degrades the WIZ transcription factor (DC50 = 13 nM in human erythroid precursors) and upregulates fetal hemoglobin (HbF) expression (EC50 = 100 nM). By inducing WIZ proteolysis, it disrupts the γ-globin repressor complex, demonstrating promising pharmacokinetics in cynomolgus monkeys for potential β-hemoglobinopathy therapy. |
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DC67337 |
VNPP433-3β
Featured
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VNPP433-3β is a first-in-class molecular glue degrader that simultaneously targets androgen receptor (AR), its splice variants (AR-Vs), and Mnk1/2 kinases for proteasomal degradation. This multimodal agent demonstrates potent anti-proliferative activity in castration-resistant prostate cancer (CRPC) models, with GI50 values of 0.2–0.31 μM in LNCaP, C4-2B, and CWR22Rv1 cells. Its robust in vivo efficacy, evidenced by tumor growth inhibition in CWR22Rv1 xenografts, is supported by favorable pharmacokinetics in CD-1 mice. |
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DC67338 |
Pan-RAS-IN-2
Featured
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Pan-rasin-2 (Compound 6A) is a novel molecular glue that selectively targets RAS, a critical oncoprotein frequently mutated in cancers. It exhibits potent anti-proliferative effects in RAS-driven cancer cell lines by disrupting oncogenic signaling. |
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DC67339 |
PLX-3618
Featured
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PLX-3618 is a targeted molecular glue that induces the degradation of BRD4, a key epigenetic regulator implicated in cancer. It achieves potent BRD4 degradation (DC50 = 12.2 nM) by recruiting the E3 ubiquitin ligase adapter DCAF11, which tags BRD4 with polyubiquitin chains for proteasome-mediated destruction. |
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DC67340 |
Naphthyridine carbamate dimer
Featured
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Naphthyridine Carbamate Dimer (NCD) is a synthetic DNA molecular glue engineered to induce programmable structural rearrangements in functional DNA. Unlike conventional small-molecule binders, NCD operates by non-covalently crosslinking specific DNA sequences, enforcing conformational changes that modulate DNA’s biological activity.
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DC67341 |
MMH2-NR
Featured
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MMH2-NR serves as an essential negative control compound for MMH2, a novel DCAF16-dependent BRD4 degrader. While MMH2 mediates targeted protein degradation by recruiting the CUL4-DCAF16 E3 ligase complex to bromodomain-containing protein 4 (BRD4), MMH2-NR is structurally analogous but lacks degradation activity, making it critical for mechanistic validation. |
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DC67342 |
BRD4 degrader-1
Featured
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BRD4 Degrader-1 (Compound ML 1-50) represents a novel class of monovalent, covalent molecular glues that selectively degrade bromodomain-containing protein 4 (BRD4) through an E3 ligase-dependent mechanism. Unlike traditional bivalent PROTACs, this compound utilizes a unique covalent binding strategy to recruit the DCAF16 E3 ubiquitin ligase, inducing potent degradation of both BRD4 long (BRD4-L) and short (BRD4-S) isoforms in cellular systems. |
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DC67343 |
DS17
Featured
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DS17 is a high-efficiency molecular glue degrader that specifically induces the degradation of cyclin K, demonstrating remarkable potency with an EC50 of 13 nM. By exploiting the ubiquitin-proteasome system, DS17 effectively eliminates cyclin K, a critical regulator of transcription and cell cycle progression, positioning it as a valuable tool in cancer research and drug discovery. |
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