STAT6 Inhibitor

Tofacitinib citrate (Standard) (Tasocitinib citrate (Standard); CP-690550 citrate (Standard)) is the analytical standard of Tofacitinib citrate (HY-40354A). This product is intended for research and analytical applications. Tofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

15 (R)-Lipoxin A4 (15-epi-LXA4) is a specialized pro-resolving mediator and an acetylated derivative of COX2. 15 (R)-Lipoxin A4 is present in neurons. 15 (R)-Lipoxin A4 induces the SPM synthases ALOX12 and ALOX15, as well as the pro-resolving receptor ALX. 15 (R)-Lipoxin A4 inhibits protein kinases, including JNK1/2/3, Lyn, STAT-3 and STAT-6. 15 (R)-Lipoxin A4 enhances the release of pro-resolving mediators. 15 (R)-Lipoxin A4 alleviates the pro-inflammatory phenotype of tendon-derived stromal cells. 15 (R)-Lipoxin A4 promotes the resolution of neuroinflammation. 15 (R)-Lipoxin A4 is applicable to research related to achilles tendinitis, achilles tendon rupture and Alzheimer’s disease.

Nitroaspirin (NCX 4016) is an orally active inhibitor of ARG1 and NOS2. Nitroaspirin reduces ARG1 enzymatic activity via the STAT6-mediated signaling pathway, and feedback-inhibits the catalytic activity of NOS2 in a NO-releasing group-dependent manner. Nitroaspirin continuously releases intracellular NO, inducing redox-dependent loss of cell viability. Nitroaspirin also exerts anti-angiogenic effects by causing endothelial barrier dysfunction, and effectively inhibits the proliferation of Cisplatin (HY-17394)-resistant human ovarian cancer cells. Nitroaspirin can be used in research related to colon cancer, breast cancer and Cisplatin-resistant human ovarian cancer.

Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

YYSW001 is a selective and orally acrive JAK1 inhibitor with an IC₅₀ of 6 nM and a Kd of 32.32 μM. YYSW001 blocks JAK1-dependent phosphorylation of STAT6, as well as IL-6-induced phosphorylation of STAT3. YYSW001 suppresses pro-inflammatory cytokine levels, reduces paw swelling, lowers clinical arthritis scores, alleviates joint damage and decreases bone loss. YYSW001 is applicable for the research of rheumatoid arthritis.

(14S,15R)-14-Deoxyoxacyclododecindione (Compound 3) acts as an inhibitor of TGF-β-dependent Smad2/3 and IL-4-dependent STAT6, with IC₅₀ values of 90 nM and 20 nM, respectively. (14S,15R)-14-deoxyoxacyclododecindione is a potent IL-4 inhibitor with an IC₅₀
value of 20 nM. (14S,15R)-14-Deoxyoxacyclododecindione is applicable to the research of chronic inflammation and fibrotic diseases.

STAT6-IN-11 is a STAT6 inhibitor with an EC₅₀ of 0.006 μM. STAT6-IN-11 can be used for the research of dermatological condition or respiratory conditions.

Tofacitinib-¹³C,d₃ (Tasocitinib-¹³C,d₃; CP-690550-¹³C,d₃) is the deuterated, ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

STAT6-IN-7 is a STAT6 inhibitor. STAT6-IN-7 exhibits an IC₅₀ of 0.28 μM for inhibiting the binding of human STAT6/pIL-4Rα. STAT6-IN-7 can be used in the research of atopic dermatitis.

STAT6-IN-8 is a STAT6 inhibitor with an IC₅₀ of 0.45 μmol/L. STAT6-IN-8 exhibits potential anti-inflammatory and anti-allergic effects. STAT6-IN-8 can be used for the research of atopic dermatitis.

STAT6-IN-9 is a potent STAT6 inhibitor with an EC₅₀ value of 4 nM. STAT6-IN-9 effectively blocks STAT6 activation mediated by the IL-13-IL-13 receptor/IL-4 receptor pathway. STAT6-IN-9 inhibits CCL17 secretion with an IC₅₀ value of 4.6 nM. STAT6-IN-9 can be used to investigate various chronic inflammatory diseases mediated by STAT6, such as allergy, asthma, and chronic obstructive pulmonary disease.

STAT6-IN-12 is a potent STAT6 inhibitor with an IC₅₀ of 50 nM. STAT6-IN-12 also inhibits Smad2/3 with an IC₅₀ of 68 nM. STAT6-IN-12 inhibits TGFβ-dependent Smad2/3 signaling pathway, IL-4-dependent STAT6 signaling pathway, and cellular inflammatory responses. STAT6-IN-12 can be used for the research of inflammation.

Tofacitinib-¹³C₃,¹⁵N (Tasocitinib-¹³C₃,¹⁵N; CP-690550-¹³C₃,¹⁵N) is the ¹⁵N, ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

STAT6-IN-13 (Compound 22) is a STAT6 inhibitor with IC₅₀ values of ≤300 nM. STAT6-IN-13 has weak inhibitory for STAT3. STAT6-IN-13 can be used for the researches of cancer, inflammation and immunology.

Tofacitinib hydrochloride (Tasocitinib hydrochloride) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib hydrochloride blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib hydrochloride can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

Tofacitinib-¹³C (Tasocitinib-¹³C; CP-690550-¹³C) is the ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

Tofacitinib-d₃ (Tasocitinib-d₃; CP-690550-d₃) is the deuterated-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

STAT6-IN-14 is a STAT6 inhibitor that blocks the binding of STAT6-pIL-4Rα, with an IC₅₀ of 1.20 μM. STAT6-IN-14 can inhibit IL-4-induced STAT6 transcriptional activity in STAT6-HEK293 cells. STAT6-IN-14 can be used for research on allergic diseases and inflammation.