JAK Inhibitor

Deucravacitinib-¹³C,d₃ is the ¹³C- and deuterium labeled Deucravacitinib. Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC₅₀=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis.

JAK2-IN-26 is a JAK2 inhibitor with an EC₅₀ greater than 0.01 μM and less than or equal to 0.05 μM. JAK2-IN-26 exhibits antiproliferative activity against cells expressing JAK2 V617F. JAK2-IN-26 can be used for research on myeloproliferative disorders.

Bufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3^tyr705, p-Stat3^ser727 and Jak2 expressions. Bufothionine upregulates Atg5, Atg7 and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer.

INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma.

Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC₅₀ value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.

JAK1/2-IN-2 (Compound 37) is a potent and selective JAK1/2 inhibitor with K_i values of 2 and 0.6 nM .

JAK-IN-37 (Compound WU4) is a JAK inhibitor, with IC₅₀ values of 0.52, 2.26, 84 and 1.09 nM for JAK1, JAK2, JAK3 and JAK4, respectively. JAK-IN-37 can be used for the research of allogeneic hematopoietic cell transplantation (allo-HCT).

Tkip is a JAK2 specific inhibitor. Tkip can bind the JAK2 autophosphorylation site, inhibit the JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip inhibits the antiviral activity of IFN-γ and the expression of MHC Class I molecules. Tkip can be used to study the IFN-γ signaling pathway.

Jak2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Jak2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

SG3-179 is a potent inhibitor against the BET bromodomain proteins. SG3-179 is also a JAK2 and FLT3 inhibitor. SG3-179 causes a rapid reduction in HOXB13 protein expression. SG3-179 is promising for research of multiple myeloma (MM1.S).

Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease.

Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis.

JAK2-IN-5 (Compound 13) is a selective JAK kinase inhibitor, with an IC₅₀ of 0.078 μM against JAK-2 and an IC₅₀ of 0.206 μM against JAK-2^V617F. JAK2-IN-5 can be used for the research of myeloproliferative disorders.

JAK3/BTK-IN-1 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002).

Tyk2-IN-17 (compound 185) is a potent TYK2 inhibitor.

Radotinib (IY-5511) dihydrochloride is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib dihydrochloride has anti-prion and anti-tumor activities. Radotinib dihydrochloride can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib dihydrochloride can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.

JAK-IN-44 is an orally active and selective JAK2 inhibitor, with IC₅₀ values of 0.2 nM, 7.3 nM, 21 nM and 27 nM against JAK2, TYK2, JAK1 and JAK3, respectively. JAK-IN-44 inhibits disease phenotypes in adjuvant-induced arthritis, systemic lupus erythematosus and experimental autoimmune uveitis models, and improves the survival rate of mice in LPS (HY-D1056)-induced sepsis models. JAK-IN-44 can be used in the research of autoimmune and inflammatory diseases such as systemic lupus erythematosus, uveitis, rheumatoid arthritis and sepsis.

Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123  µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation.

Upadacitinib-d₅ (ABT-494-d₅) is the deuterium labeled Upadacitinib (HY-19569). Upadacitinib (ABT-494) is a potent, orally active and selective JAK1 inhibitor (IC₅₀ = 43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research.

AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD).