stat6

STAT6-IN-2 (Comp R-84) is a STAT6 inhibitor that effectively reduces the secretion of the chemokine eotaxin-3, which induces eosinophil infiltration. This compound is valuable for studying immune diseases [1].

AS1517499 is a blood-brain barrier permeable inhibitor of STAT6 phosphorylation (IC50= 21 nM).

AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate for research into allergic diseases, including asthma and atopic conditions.

STAT6-IN-1, a STAT6 inhibitor, exhibits high affinity for the SH2 domain of STAT6 (IC 50 = 0.028 µM), making it suitable for research on allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer.

STAT6-IN-3 (Compound 18a) is an inhibitor of STAT6, targeting the Src Homology 2 (SH2) domain with an IC50 value of 44 nM. It is used in research on inflammatory disorders, such as asthma [1].

STAT6-IN-5 (34) is an inhibitor of STAT6 with an IC50 of 0.24 μM.

STAT6-IN-4 (78) functions as a STAT6 inhibitor, exhibiting an IC50 value of 0.34 μM.

AK-1690 is a potent and selective STAT6 PROTAC degrader that induces degradation of STAT6 proteins in cells (DC50=1 nM) and depletes STAT6 proteins in mouse tissues, which can be used in cancer research.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

AK-068 is a STAT6 ligand with a Ki value of 6 nM, exhibiting at least 85-fold higher selectivity in binding to STAT6 over STAT5.

7-Bromohept-1-yne is a PROTAC Linker that can be used to synthesize AK-1690, a STAT6 (Signal transducer and activator of transcription 6) PROTAC degradator.

SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models.

Smad2/3-IN-2 (Compound 3) is an inhibitor of the TGF-β-dependent Smad2/3 signaling pathway and the IL-4-dependent STAT6 signaling pathway, with IC50 values of 90 nM and 20 nM, respectively.

Smad2/3-IN-2 (Compound 27) is an inhibitor of the TGF-β-dependent Smad2/3 signaling pathway and the IL-4-dependent STAT6 signaling pathway, with IC50 values of 90 nM and 20 nM, respectively.

iHSP110-33 is an inhibitor of the molecular chaperone heat shock protein 110 (HSP110). This compound exhibits antitumor effects against large B-cell lymphoma and classical Hodgkin's lymphoma. It works synergistically with Selinexor, enhancing the inhibition of STAT6 phosphorylation and boosting its antitumor activity.

YM-341619 (AS1617612) is a potent, orally active STAT6 inhibitor (IC50: 0.70 nM) that inhibits IL-4-induced Th2 differentiation in mouse splenic T cells with an IC50 value of 0.28 nM, without affecting Th1 cell differentiation. YM-341619 holds potential for research into allergic diseases, such as allergic asthma.

PM-43I is a potent inhibitor of both STAT5- and STAT6-dependent allergic airway disease in mice.

PM-81I, a potent STAT6 inhibitor targeting the SH2 structural domain, effectively reduces STAT6 phosphorylation levels. It is applicable in the research of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer [1].

Rademikibart (CBP-201) is a humanised monoclonal antibody targeting IL-4Rα (KD = 20.7 pM) that does not interact with IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signalling pathways, TF-1 cell proliferation, and TARC production in PBMCs, making it useful for studying Th2-type inflammatory diseases.

7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.