JAK Inhibitor

BXL0124 is an orally effective CD44 inhibitor and Notch signaling pathway inhibitor. BXL0124 has a vitamin D receptor-dependent mechanism and can downregulate the expression of CD44, Notch1/2/3, HES1, OCT4, LAMA5, JAG1, JAG2, NF-κB and DLL1. BXL0124 inhibits c-Myc expression and the levels of phosphorylated ERK, AKT, ErbB2, reduces the level of activated Notch1 receptor and its nuclear localization, decreases the mRNA and protein levels of Jagged-1 and Jagged-2, and inhibits the STAT3 signaling pathway by reducing the formation of the CD44-STAT3-JAK2 complex, while also inhibiting the transcriptional activity of the CD44 promoter in a p53-dependent manner. BXL0124 can induce myoepithelial differentiation and inhibit the self-renewal of cancer stem cell-like cells, cancer cell proliferation, invasion, and growth. BXL0124 can be used in research related to triple-negative breast cancer, basal-like breast cancer, ErbB2-overexpressing mammary tumorigenesis, and breast cancer.

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.

Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

Filgotinib (maleate) (Standard) is the analytical standard of Filgotinib (maleate). This product is intended for research and analytical applications. Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values ​​of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.

ZM39923 is a JAK3 inhibitor, with a pIC₅₀ of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.

AG490 (Standard) is the analytical standard of AG490 (HY-12000). This product is intended for research and analytical applications. AG490 (Tyrphostin AG490) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Tyk2-IN-14 is a Tyk2 inhibitor that regulates IFNα and IL-23 by inhibiting Tyk2-mediated signal transduction. Tyk2-IN-14 exhibits an IC₅₀ of 0.08 μM against the IL-23 Kit225 reporter gene and an IC₅₀ of 0.09 μM against the IFNα Kit225 reporter gene. IL-23 modulator-1 is applicable to the research of inflammatory diseases and autoimmune diseases.

Iridin (Standard) is the analytical standard of Iridin. This product is intended for research and analytical applications. Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.

AH057 is an orally active JAK1 and JAK2 inhibitor. AH057 blocks IL-6-, IFN-α- and IFN-γ-induced JAK/STAT signaling, reduces cancer cell proliferation, invasion and colony formation, and induces apoptosis and G1 cell-cycle arrest. AH057 can be used for cervical cancer research.

CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and JAK3.

Momelotinib (Standard) is the analytical standard of Momelotinib. This product is intended for research and analytical applications. Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

NMS-P953 (compound 28) is an orally active JAK2 inhibitor (IC₅₀=0.008 μM) with antitumor activity.

Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML).

CT 2576 is a phospholipid signaling inhibitor as well as a Jak3/STAT5 inhibitor. CT 2576 suppresses gene expression and replication of human immunodeficiency virus (HIV) at the post-transcriptional level by interfering with phospholipid metabolism in host cells, particularly by inhibiting the production of phosphatidic acid PA. CT-2576 completely inhibits the growth and proliferation of malignant T-cell lymphoma cells by suppressing phospholipid signaling and blocking the Jak/STAT signaling pathway associated with IL-2R. CT 2576 can be used in research related to human immunodeficiency virus (HIV) infection and cutaneous T-cell lymphoma (CTCL).

BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the JAK2-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research.

Momelotinib (sulfate) (Standard) is the analytical standard of Momelotinib (sulfate). This product is intended for research and analytical applications. Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).

Linderane (Standard) is the analytical standard of Linderane (HY-N0688). This product is intended for research and analytical applications. Linderane is an orally active natural sesquiterpene lactone with blood-brain barrier permeability. Linderane indirectly activates PDE3 by activating ERK/STAT3, thereby inhibiting the cAMP/PKA/CREB signaling pathway and hepatic gluconeogenesis. Linderane protects pancreatic β cells against oxidative damage by inhibiting the activation of the p38 MAPK pathway and activating the Nrf2 pathway. Linderane inhibits cell apoptosis and ameliorates intestinal mucosal inflammation by suppressing the IL-6/JAK/STAT3 signaling pathway. Linderane reduces pain sensitivity and alleviates anxiety-like behaviors by activating cannabinoid receptor 2 (CB2R). Linderane can be used in studies related to type 2 diabetes, ulcerative colitis, and chronic inflammatory pain with anxiety.

SAR-20347 (Standard) is the analytical standard of SAR-20347 (HY-100895). This product is intended for research and analytical applications. SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.

R-348 (R-932348) choline is a potent and orally active JAK3 and Syk inhibitor. R-348 reduces IFN-γ, IL-6, and IL-10 expression. R-348 effectively diminishes acute cardiac allograft rejection.