STAT1 Inhibitor

Tofacitinib (Standard) (Tasocitinib (Standard); CP-690550 (Standard)) is the analytical standard of Tofacitinib (HY-40354). This product is intended for research and analytical applications. 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.

Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra chinensis with oral availability. Gomisin M2 inhibits STAT1 phosphorylation as well as NF-κB p65 phosphorylation and nuclear translocation. Gomisin M2 reduces inflammatory cell infiltration, cytokine and chemokine expression, and serum IgE and IgG_2a levels. Gomisin M2 inhibits MAPK phosphorylation, IκBα degradation, and NF-κB nuclear translocation in keratinocytes. Gomisin M2 induces apoptosis, mitochondrial membrane potential disruption, and cytochrome c release, and inhibits DNA synthesis and mammosphere formation through downregulation of Wnt/β-catenin. Gomisin M2 can be used for research on atopic dermatitis, psoriasis, breast cancer, liver injury, and multidrug-resistant mammary adenocarcinoma.

Tofacitinib-d₃ citrate (Tasocitinib-d₃ citrate; CP-690550-d₃ citrate) is the deuterated-labeled Tofacitinib citrate (HY-40354A). 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.

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.

Itacitinib adipate (INCB039110 adipate) is an orally active JAK1-selective inhibitor. Itacitinib adipate inhibits IFN-γ-mediated phosphorylation of STAT1 and downstream pro-inflammatory signaling pathways. Itacitinib adipate reduces the frequency and number of splenic neutrophils in mouse models, downregulates the levels of pro-inflammatory cytokines and chemokines, and inhibits pro-inflammatory gene expression pathways. Itacitinib adipate improves survival rate and clinical scores in mouse models of hemophagocytic lymphohistiocytosis (HLH), and also suppresses metastasis in NSCLC models with high Rab1A expression. Itacitinib adipate can be used for research on hemophagocytic lymphohistiocytosis and non-small cell lung cancer.

IFN-α Receptor Recognition Peptide 1 (IRRP1) is an amino acid synthetic peptide and also a regulator of IFN-α Receptor. IFN-α Receptor Recognition Peptide 1 binds to IFNAR2, enhances the binding capacity of IFN-α receptor, and slightly increases the IFN-α-induced growth inhibitory activity. IFN-α Receptor Recognition Peptide 1 inhibits IFN-α-induced STAT1 phosphorylation and STAT-DNA binding by blocking the activation of IFNAR by IFN-α. IFN-α Receptor Recognition Peptide 1 increases the occupancy of IFN-α on cell surface receptors, enhances the phosphorylation activation of ISGF3, and elevates IFN-α-induced antiviral activity. IFN-α Receptor Recognition Peptide 1 can be used in studies related to encephalomyocarditis virus infection.

IFN-α Receptor Recognition Peptide 1 acetate (IRRP1 acetate) is an amino acid synthetic peptide and also a regulator of IFN-α Receptor. IFN-α Receptor Recognition Peptide 1 acetate binds to IFNAR2, enhances the binding capacity of IFN-α receptor, and slightly increases the IFN-α-induced growth inhibitory activity. IFN-α Receptor Recognition Peptide 1 acetate inhibits IFN-α-induced STAT1 phosphorylation and STAT-DNA binding by blocking the activation of IFNAR by IFN-α. IFN-α Receptor Recognition Peptide 1 acetate increases the occupancy of IFN-α on cell surface receptors, enhances the phosphorylation activation of ISGF3, and elevates IFN-α-induced antiviral activity. IFN-α Receptor Recognition Peptide 1 acetate can be used in studies related to encephalomyocarditis virus infection.

Biflorin has antimicrobial, antitumor, antiinflammatory and antimutagenic activities. Biflorin is found in the roots of Capraria biflora L.

UT-105 is an orally active, selective androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR, inhibits the transactivation of AR, blocks the recruitment of AR to androgen response elements, and induces AR degradation. UT-105 inhibits the JAK-STAT signaling pathway, including reducing the expression of interferon-stimulated genes, inhibiting the phosphorylation of STAT1 and STAT3, and blocking the recruitment of STAT1 to response elements. UT-105 exhibits anticancer activity against AR-positive triple-negative breast cancer (TNBC). UT-105 can be used in the research of selective androgen receptor modulator-resistant ER-positive breast cancer and triple-negative breast cancer.

CDK8-IN-2 is an orally active CDK8 inhibitor of an IC₅₀ values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC₅₀ value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.

GG13 is an anti-inflammatory peptide. GG13 reduces the expression of STAT1, NOS2, COX2, and CD40. GG13 decreases the expression and secretion of iNOS and TNF-α proteins. GG13 is applicable to the research of inflammatory diseases.

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.

ITA-5 is a TBK1 inhibitor based on the structure of itaconic acid. can significantly inhibit the secretion of IFN-β. ITA-5 can inhibit the phosphorylation of TBK1, IRF3, and STAT1. ITA-5 can be used for research on autoimmune diseases and excessive inflammation.

Apoptosis inducer 55 (Compound 10) is an Apoptosis inducer. Apoptosis inducer 55 induces rapid apoptosis via the intrinsic pathway. Apoptosis inducer 55 potently inhibits several signaling cascades including AKT, ERK1/2, STAT1, STAT3, and S6K. Apoptosis inducer 55 has anti-cancer activity against melanoma.

Orazipone (OR 1384) is a small molecule immunomodulator with strong anti-inflammatory properties. Orazipone exerts its immunomodulatory effect by forming reversible thiol complexes, which bind to intracellular signaling proteins and the thiol groups of glutathione. Orazipone exhibits potent anti-eosinophilic activity by inducing apoptosis. Orazipone inhibits activation of inflammatory transcription factors NF-kB and STAT 1 and decreases inducible iNOS expression and NO production in response to inflammatory stimuli. Orazipone reduces NADPH oxidase activity and thereby decreases ROS production. Orazipone has a protective effect in intestinal radiation injury.

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.

JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.

KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.

SNX631 is an orally active and selective CDK8/CDK19 inhibitor. SNX631 reduces the phosphorylation of STAT1/STAT3 S727, and upregulates miR-21-5p, miR-21-3p and miR-221 in cancer cells. SNX631 transcription-independently inhibits meiotic resumption in mouse oocytes, blocks nuclear envelope breakdown, first polar body extrusion and mitochondrial expansion and aggregation, with no cytotoxicity. SNX631, in combination with Lapatinib (HY-50898) or Trastuzumab (HY-P9907), synergistically inhibits cancer cell growth, upregulates the tumor suppressor BTG2, prevents Lapatinib-induced upregulation of oncogenic miRNAs, overcomes drug resistance, reduces the infiltration of αSMA+ stromal fibroblasts and ARG1+ M2 macrophages, and exhibits favorable biosafety. SNX631 can be used in studies related to HER2-positive breast cancer and cancer.

ISS840 is a selective STAT1 inhibitor, with an IC₅₀ of 31 μM against STAT1 and an IC₅₀ of 560 μM against STAT3. ISS840 is applicable for cancer research.