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.

NRX-252262 is a powerful enhancer of the interaction between β-Catenin and its cognate E3 ligase, SCFβ-TrCP. It effectively induces the degradation of mutant β-catenin, demonstrating an EC50 of 3.8 nM.

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.

Voclosporin (ISAtx-247) is an inhibitor of calcineurin (PP2B), also known as CN, exhibiting its activity through targeted suppression of this enzyme.

ALV2 is a potent and selective degrader of Helios, a zinc-finger transcription factor crucial for maintaining a stable regulatory T-cell (Treg) phenotype in inflammatory tumor microenvironments. ALV2 binds to CRBN with an IC50 of 0.57 μM, demonstrating its specificity and efficacy.

Avadomide is an orally bioavailable cereblon modulator that regulates cereblon E3 ligase activity, inhibits the NF-κB pathway, and induces cell cycle arrest at the G1 phase, leading to apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. It demonstrates significant antitumor and immunomodulatory effects.

FPFT-2216 is a "molecular glue" compound that induces the degradation of phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), and casein kinase 1α (CK1α). It holds potential for research in cancer and inflammatory diseases.

Golcadomide (CC-99282) is a highly potent and orally bioavailable CRBN E3 ligase modulator (CELMoD). It interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, facilitating the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide holds significant promise for research in cancer-related areas, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).

CFT7455 is an orally bioavailable degrader of the zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). It functions as an anticancer agent by binding with high affinity to the cereblon E3 ligase, exhibiting a Kd of 0.9 nM (WO2022032132A1; Compound 1).

TMX-4116 is a potent degrader of casein kinase 1α (CK1α), demonstrating strong degradation activity with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cell lines. It holds significant potential for research applications in multiple myeloma.

NVP-DKY709 is a powerful IKZF2 inhibitor with significant potential for cancer therapy.

BI-3802 (BI3802) is a highly potent and effective BCL6 degrader that disrupts the interaction between the BTB/POZ domain of BCL6 and its co-repressors in vitro, achieving an IC50 of less than 3 nM.

E7820 is an angiogenesis inhibitor that exerts its effects by targeting integrin α2, a cell adhesion molecule prominently expressed on endothelial cells.

SJ6986 is a highly potent, selective, and orally bioavailable degrader of GSPT1/2, with a DC50 of 2.1 nM. It exhibits strong antiproliferative effects in MV4-11 and MHH-CALL-4 cell lines, showing IC50 values of 1.5 nM and 0.4 nM, respectively.