PROTAC(H-PGDS)-7 represents a breakthrough in targeted protein degradation, achieving ​unprecedented picomolar efficacy (DC50 = 17.3 pM) against hematopoietic prostaglandin D synthase (H-PGDS).

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.

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).

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.

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.

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.

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.

(Rac)-CFT7455 is a potent, racemic small-molecule degrader of the zinc finger transcription factors ​IKZF1 (Ikaros) and IKZF3 (Aiolos), operating through ​ubiquitin-proteasome-mediated degradation. It demonstrates exceptional cellular potency, with a ​GI50 of 0.05 nM in NCI-H929.1 cells. As the racemic form of ​CFT7455, it retains the same ​anticancer activity by selectively targeting IKZF1/3 for proteasomal destruction.

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).

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.

SJPYT-195 is a potent cytotoxic degrader of GSPT1, serving as a valuable compound for PROTAC (proteolysis-targeting chimera) synthesis and targeted protein degradation research.

IBG3 is a PROTAC-like degrader that exhibits superior degradation efficiency for BRD4 and BRD2 compared to IBG1, with DC50 values of 6.7 pM and 8.6 pM, respectively.

TMX-4113 is a degrader targeting phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). It is a valuable tool for cancer research.

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.

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.

Biotin-Thalidomide serves as a cereblon affinity probe, widely used in PROTAC and targeted protein degradation research.

CCT369260 (compound 1) is an orally active inhibitor of B-cell lymphoma 6 (BCL6) with significant anti-tumor activity. It demonstrates an IC50 value of 520 nM.

(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-enantiomer of Thalidomide, known for its immunomodulatory, anti-inflammatory, antiangiogenic, and pro-apoptotic properties. It induces teratogenic effects through its binding to cereblon (CRBN).

CCT373566 is a highly potent, in vivo active BCL6 degrader, demonstrating an IC50 of 2.2 nM in TR-FRET assays and a DC50 of 0.7 nM in cellular BCL6 degradation assays.

Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analog of sulfaquinoxaline, acts as a topoisomerase II alpha/beta poison. It is utilized to manage coccidiosis in poultry, rabbits, sheep, and cattle, while also demonstrating antitumor activity.

TMX-4100 is a selective degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation efficiency with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cells. It is a promising compound for research in multiple myeloma.

ZXH-1-161 is a potent cereblon (CRBN) modulator, demonstrating an IC50 value of 39 nM in MM1.S wild-type cells. It exhibits selective degradation activity toward GSPT1 and is a valuable tool for researching multiple myeloma.

NRX-252114 is a potent enhancer of the interaction between β-catenin and its cognate E3 ligase, SCFβ-TrCP. It significantly strengthens the binding of the pSer33/S37A β-catenin peptide to β-TrCP, exhibiting an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 also induces the degradation of mutant β-catenin.

NCT02 is a small molecule that triggers the ubiquitination of cyclin K (CCNK), leading to its proteasomal degradation along with its complex partner CDK12.

Schisandrin C (Schizandrin-C) is a phytochemical lignan derived from Schizandra chinensis, known for its diverse biological activities, including anticancer, anti-inflammatory, and antioxidant effects. Functioning as a molecular glue, Schisandrin C holds potential for research in cancer, Alzheimer’s disease, and liver diseases. It also induces cell apoptosis.

NRX-103094 is a potent enhancer of the interaction between β-catenin and its cognate E3 ligase, SCFβ-TrCP. It significantly strengthens the binding of the pSer33/Ser37 β-catenin peptide to β-TrCP, exhibiting an EC50 of 62 nM and a Kd of 0.6 nM.

NVS-STG2 is a molecular glue that targets STING and activates STING-mediated immune signaling. It promotes higher-order oligomerization of human STING by binding to pockets between adjacent STING dimer transmembrane domains, effectively functioning as a molecular glue. NVS-STG2 enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. It demonstrates significant antitumor activity in animal models.

Tasisulam is an anticancer agent that triggers apoptosis through the intrinsic pathway, leading to cytochrome c release and caspase-dependent cell death. It also inhibits mitotic progression and promotes vascular normalization.

(R)-CR8 trihydrochloride (CR8 trihydrochloride), a second-generation derivative of Roscovitine, is a highly potent inhibitor of CDK1/2/5/7/9. It exhibits inhibitory activity against CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM), and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and demonstrates neuroprotective properties.