Sibeprenlimab (VIS649) is a humanized IgG2 monoclonal antibody which inhibits a proliferation-inducing ligand (APRIL). Sibeprenlimab suppresses pathogenic immunoglobulins (IgA and IgM), while preserving antibody responses to mRNA-based vaccines against SARS-COV-2. Sibeprenlimab reduces urinary protein-to-creatinine ratio (UPCR) and glomerular filtration rate (GFR). Sibeprenlimab is promising for the research of IgA nephropathy (IgAN).

Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab (HY-P9913). Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL).

Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20+ non-Hodgkin lymphomas (NHL).

Brentuximab is a monoclonal antibody targeting CD30. Brentuximab is conjugated with monomethyl auristatin E (MMAE) (HY-15162) to form the antibody-drug conjugate Brentuximab vedotin (HY-P99107), which can induce apoptosis in primary effusion lymphoma cells. Brentuximab vedotin exhibits antitumor activity with an IC50 of 10 nM against human CD30+ cancer cells.

Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity.

Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment.

Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: ?0.24?nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection.

Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases.

AV-105 is a tosylate precursor compound derived from ​Florbetapir (18F), a radiolabeled styrylpyridine derivative referenced in ​patent WO2010078370A1 (Example 1.5). This precursor plays a crucial role in the synthesis of ​18F-radiolabeled imaging agents, particularly for ​positron emission tomography (PET) applications.

AZ-5104 is a pharmacologically active metabolite derived from the demethylation of ​AZD9291 (osimertinib). It functions as a ​potent EGFR inhibitor, demonstrating strong inhibitory activity against various ​EGFR mutants and ​ErbB4.

ML162 is a covalent inhibitor that specifically targets ​glutathione peroxidase 4 (GPX4), a key regulator of ferroptosis. This compound exhibits ​selective cytotoxicity against cancer cell lines harboring ​mutant RAS oncogenes, making it a promising candidate for precision oncology.

A83B4C63 is a highly potent small-molecule inhibitor targeting the DNA repair enzyme polynucleotide kinase 3'-phosphatase (PNKP), exhibiting strong binding affinity with a ​Kd of 80 nM. Due to its limited aqueous solubility, A83B4C63 was formulated into ​nano-encapsulated carriers, enhancing its therapeutic potential—particularly in ​PTEN-deficient colorectal cancer (CRC).

Furamidine dihydrochloride (NSC 305831) tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.

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.