DC67376 |
GSPT1 degrader-1
Featured
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GSPT1 degrader-1 (compound 9q) is a potent molecular glue that mediates targeted degradation of G1-to-S phase transition protein 1 (GSPT1) through the ubiquitin-proteasome pathway. This compound exhibits dual biological activity by inducing cell cycle arrest at the G0/G1 phase checkpoint and triggering apoptotic signaling cascades. |
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DC67377 |
JP-2-249
Featured
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JP-2-249 functions as a molecular glue degrader that selectively targets SMARCA2 for proteasomal degradation. In MV-4-11 leukemia cells, treatment with JP-2-249 (1–10 μM) induces dose-dependent reduction of SMARCA2 protein levels, demonstrating potent degradation activity. |
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DC67378 |
GSPT1 degrader-2
Featured
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GSPT1 degrader-2 (Compound 210) is an orally bioavailable molecular glue that achieves potent, sub-30 nM degradation of GSPT1 (DC50 < 30 nM), demonstrating robust antitumor efficacy in preclinical models. |
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DC67379 |
STING Degrader-1
Featured
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STING Degrader-1 (compound 2) is a covalent molecular glue that simultaneously engages STING and its cognate E3 ligase, inducing targeted protein degradation. The compound exhibits a characteristic hook effect, achieving maximal STING depletion (75%) at 10 μM, while higher concentrations (30 μM) show reduced degradation efficiency (~30%). |
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DC67380 |
CQ627
Featured
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CQ627 is a targeted molecular glue that promotes RIOK2 degradation through the ubiquitin-proteasome pathway by bridging interactions between RIOK2 and the E3 ligase RNF126, achieving a DC50 of 410 nM in MOLT4 leukemia cells. This compound demonstrates multi-modal anticancer activity, including: (1) dose-dependent apoptosis induction, (2) G2/M phase cell cycle arrest, and (3) broad-spectrum antiproliferative effects across cancer cell lines. Furthermore, CQ627 shows significant in vivo efficacy in MOLT4 xenograft models, validating its therapeutic potential. |
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DC67381 |
Z-NCTS
Featured
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Z-NCTS is a sequence-selective RNA-binding molecule that specifically targets 5’-r(XGG)-3’/5’-r(XGG)-3’ mismatches (where X = U or A), functioning as a molecular glue to stabilize these RNA duplex structures. |
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DC67382 |
IKZF1-degrader-2
Featured
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IKZF1-degrader-2 (Compound 3) is a targeted molecular glue that induces selective degradation of IKZF1, demonstrating potent anticancer efficacy with an advantageous safety profile. |
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DC67383 |
UNC8732
Featured
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UNC8732 is a dual-functional compound that both inhibits and degrades NSD2, offering a two-pronged approach to targeting this epigenetic regulator. |
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DC67384 |
CDK4 degrader 1
Featured
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CDK4 degrader 1 (ML 1–71) is a molecular glue compound that selectively induces cyclin-dependent kinase 4 (CDK4) degradation through targeted ubiquitin-proteasome system recruitment. |
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DC67385 |
BRD9 Degrader-3
Featured
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BRD9 Degrader-3 (compound B20) is a highly potent molecular glue that induces targeted BRD9 degradation, demonstrating exceptional activity with a DC50 below 1.25 nM. |
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DC67386 |
UNC8732 TFA
Featured
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UNC8732 (TFA salt) is a bifunctional agent that simultaneously inhibits NSD2 methyltransferase activity and promotes its targeted degradation, offering dual epigenetic modulation. |
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DC67387 |
XYD049
Featured
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XYD049 (compound 7d) is a CRBN-recruiting molecular glue that selectively degrades GSPT1 with high potency (DC50 = 19 nM), demonstrating therapeutic potential against MYC-driven castration-resistant prostate cancer (CRPC). |
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DC67388 |
GR–14-3-3 stabilizer-1
Featured
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GR-14-3-3 stabilizer-1 (compound 10) is a molecular glue designed to reinforce the glucocorticoid receptor (GR)-14-3-3 protein interaction. By selectively stabilizing this complex, it effectively disrupts GR signaling and serves as a versatile scaffold for developing targeted molecular glues. |
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DC67389 |
GSPT1 degrader-6
Featured
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GSPT1 degrader-6 (compound 8) is a highly potent molecular glue that induces targeted degradation of GSPT1, demonstrating exceptional activity with a DC50 of 13 nM. |
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DC67390 |
Pan-RAS-IN-5
Featured
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Pan-RAS-IN-5 (compound 7A) is a molecular glue that induces a functional ternary complex between cyclophilin A (CYPA) and activated RAS (RAS-ON), effectively disrupting RAF recruitment and downstream signaling. This unique mechanism translates to potent anti-tumor activity. |
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DC67391 |
WIZ degrader 8
Featured
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WIZ degrader 8 (compound 10) is a potent and selective molecular glue that induces targeted degradation of the transcription factor WIZ, resulting in robust upregulation of fetal hemoglobin (HbF) expression. This dual activity—WIZ depletion coupled with HbF induction—positions it as a promising therapeutic candidate for sickle cell disease. |
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DC67392 |
PROTAC GSPT1 degrader-2
Featured
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PROTAC GSPT1 degrader-2 (compound A) is a highly efficient molecular glue that achieves near-complete GSPT1 degradation (>95%). This compound demonstrates potent anti-proliferative activity in HL-60 leukemia cells, with an IC50 value of 10 nM, highlighting its therapeutic potential. |
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DC67393 |
Pomalidomide-d5
Featured
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Pomalidomide-d5 is a deuterium-stabilized isotopologue of pomalidomide, a third-generation immunomodulatory drug that functions as a molecular glue degrader. This compound mediates targeted protein degradation by recruiting the cereblon E3 ubiquitin ligase to promote ubiquitination and proteasomal elimination of Ikaros family transcription factors (IKZF1/3), a mechanism central to its therapeutic activity. |
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DC67394 |
HGC652
Featured
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HGC652 is a first-in-class molecular glue that selectively recruits the E3 ubiquitin ligase TRIM21 to form a ternary complex with NUP98, triggering targeted degradation of NUP155 and nuclear pore complex (NPC) proteins. This unique mechanism induces potent cytotoxicity across multiple cancer types, with activity correlating with cellular TRIM21 expression levels. |
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DC67395 |
Cyclosporin A-d3
Featured
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Cyclosporin A-d3 is a deuterium-enriched isotopologue of Cyclosporin A (HY-B0579), designed for metabolic stability studies and quantitative mass spectrometry applications. |
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DC67396 |
CDK-IN-9
Featured
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CDK-IN-9 (compound 24) is a bifunctional agent that combines potent CDK2/E inhibition (IC50 = 4 nM) with molecular glue activity, selectively bridging CDK12 and DDB1 to trigger polyubiquitination and proteasomal degradation of cyclin K. |
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DC67397 |
JWJ-01-306
Featured
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JWJ-01-306 is a first-in-class molecular glue that selectively targets and degrades the C2H2 zinc finger transcription factor ZBTB11, disrupting mitochondrial metabolism by suppressing oxidative phosphorylation (OXPHOS) and the tricarboxylic acid (TCA) cycle. This dual metabolic reprogramming activity overcomes proliferation in KAS-mutant pancreatic ductal adenocarcinoma (PDAC) cells while demonstrating favorable pharmacokinetic properties in vivo. |
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DC67398 |
SJ46411-Br
Featured
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SJ46411-Br is a selective CRL2^KLHDC2 E3 ligase ligand that facilitates cooperative, target-specific ternary complex formation. Its modular design enables conjugation to BET inhibitors like JQ1 (HY-13030) via PROTAC linkers, serving as a versatile scaffold for developing KLHDC2-directed degraders. |
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DC67399 |
VAV1 degrader-2
Featured
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VAV1 degrader-2 (Example 176) is a high-potency molecular glue that selectively targets VAV1 for degradation (DC50 = 4.41 nM), demonstrating therapeutic potential for modulating inflammatory and autoimmune pathways. |
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DC67400 |
ER degrader 9
Featured
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ER degrader 9 (compound 1) is a bifunctional molecular glue that achieves sub-10 nM degradation potency (DC50 ≤10 nM) against estrogen receptor (ER) in MCF-7 breast cancer cells, demonstrating significant potential for therapeutic development in ER-dependent malignancies. |
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DC67401 |
GSPT1 degrader-5
Featured
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GSPT1 degrader-5 (compound 4) is a molecular glue compound that induces targeted degradation of GSPT1 with a DC50 of 144 nM, demonstrating moderate but selective activity. |
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DC67402 |
Pomalidomide-15N,13C5
Featured
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Pomalidomide-15N,13C5 is a stable isotope-labeled variant of pomalidomide (HY-10984), a third-generation immunomodulatory drug that functions as a cereblon-directed molecular glue. This compound mediates targeted ubiquitination and degradation of Ikaros family transcription factors (IKZF1/3) through recruitment of the CRL4CRBN E3 ligase complex, underpinning its therapeutic mechanism. |
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DC67403 |
KRAS ligand 4
Featured
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KRAS ligand 4 (compound 2) is a SOS1-targeting bifunctional molecular glue that suppresses oncogenic signaling by degrading key KRAS pathway components, evidenced by reduced pERK and pS6 levels. It demonstrates broad-spectrum activity against diverse KRAS mutations, disrupting proliferation across resistant cancer models. |
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DC67404 |
QS-57
Featured
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QS-57 is a bifunctional degrader that combines BRD4-targeting PROTAC activity with 14-3-3 molecular glue properties. |
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DC67405 |
Acetyl-cyclosporin A aldehyde
Featured
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Acetyl-cyclosporin A aldehyde is a chemically modified derivative of cyclosporin A (HY-B0579), featuring an acetyl group and a reactive aldehyde moiety. The parent compound, cyclosporin A, is a dual-function molecule that both inhibits calmodulin signaling and binds cyclophilin, thereby blocking NF-AT nuclear translocation and inducing mitochondrial dysfunction. |
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