Pyrinuron is an inhibitor of NAMPT and NMNAT2.Pyrinuron is used as a model compound in studies of urea derivatives and their reactivity.Research has explored the effects of this compound on insulin-producing beta cells, providing insights into diabetes mechanisms.Although not used therapeutically, this compound’s ability to selectively destroy beta cells has implications for understanding and potentially treating type 1 diabetes.

IKZF1-degrader-1 (Compound 9-B) is a highly potent molecular glue that achieves sub-nanomolar degradation of IKZF1 (DC50 = 0.134 nM), demonstrating significant therapeutic potential for targeting IKZF1-dependent malignancies.

EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity.

EM12-FS is a bifunctional CRBN modulator that engages cereblon at His353 while functioning as a molecular glue to induce NTAQ1 degradation. Demonstrating favorable pharmacokinetics, it exhibits a human plasma half-life of 196 minutes, supporting its therapeutic potential.

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.

QS-57 is a bifunctional degrader that combines BRD4-targeting PROTAC activity with 14-3-3 molecular glue properties.

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.

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.

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.

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.

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.

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.

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.

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.

Cyclosporin A-d3 is a deuterium-enriched isotopologue of Cyclosporin A (HY-B0579), designed for metabolic stability studies and quantitative mass spectrometry applications.

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.

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.

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.

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.

Novel positive allosteric modulator (PAM) of the GLP-1R, enhancing insulin secretion in a glucose-, ligand- and GLP-1R-dependent manner

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.

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.

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).

UNC8732 (TFA salt) is a bifunctional agent that simultaneously inhibits NSD2 methyltransferase activity and promotes its targeted degradation, offering dual epigenetic modulation.

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.

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.

UNC8732 is a dual-functional compound that both inhibits and degrades NSD2, offering a two-pronged approach to targeting this epigenetic regulator.