JAK/STAT Signaling

Zalutumumab is a highly affinity pure human IgG1 monoclonal antibody that targets EGFR. Zalutumumab binds to domain III of the epidermal growth factor receptor, exerting its effects by blocking the binding of epidermal growth factor and interfering with the receptor's active conformation. The EC50 values for Zalutumumab with IgG and its Fab regions are 7 and 19 nM, respectively. Zalutumumab can be used in cancer research.

Zanidatamab (ZW25) is a human bispecific monoclonal antibody targeting 2 different HER2 epitopes (ECD2 and ECD4). Zanidatamab has anti-tumor activity.

Zenocutuzumab is a bispecific humanized IgG1 antibody containing two different Fab arms that target the extracellular domains of HER2 and HER3.

Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.

JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM).

Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3.

PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level.

PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels.

STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM).

Nimucitinib is a Janus kinase (JAK) inhibitor.

STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF).

PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader.

JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively.

STAT6-IN-3 (Compound 18a) is a STAT6 inhibitor (IC50= 44 nM).

Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3.

STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants.

JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM.

Deuruxolitinib, a deuterated Ruxolitinib , modulates the activity of JAK1/JAK2.

OK2, a specific inhibitor of the CCN2/EGFR interaction, efficiently blocks CCN2/EGFR interaction through binding to the CT domain of CCN2.

Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody that specifically targets Her3 (ErbB3).

Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ.

(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor.

Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5.

Erasin is a potent Erlotinib -resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively.